Home Metabolism PPAR agonist Rosiglitazone (BRL-49653)

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Rosiglitazone (BRL-49653) PPARγ Agonist

Cat.No.S2556

Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Rosiglitazone (BRL-49653) PPAR agonist Chemical Structure

Chemical Structure

Molecular Weight: 357.43

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Quality Control

Batch: Purity: 99.99%
99.99

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 Function assay Effective concentration against human PPARgamma expressed in HepG2 cells, EC50=0.02 μM 15801817
CV-1 Function assay In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50 = 0.06 μM. 8576907
CV-1 Function assay Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50 = 0.08913 μM. 9836620
3T3-L1 Function assay Stimulation of adipogenesis in 3T3-L1 cells is expressed as concentration equivalent to the [ 1-14C] uptake counts after treatment with 0.2 ug/mL troglitazone, EC = 0.09 μM. 10956213
CV-1 Function assay Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay., EC50 = 0.043 μM. 11720854
COS1 Function assay Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor, EC50 = 0.021 μM. 12617924
COS1 Function assay In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells, EC50 = 0.02 μM. 12729668
COS1 Function assay In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells, EC50 = 0.02 μM. 12873517
CV-1 Function assay In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined, EC50 = 0.325 μM. 12954061
3T3-L1 Function assay Effective concentration for enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC30 = 0.02 μM. 14505644
HepG2 Function assay Effective concentration against human PPARgamma expressed in HepG2 cells, EC50 = 0.039 μM. 16107150
U2OS Function assay Effect on PPARgamma transactivation activity in U2OS cells, EC50 = 0.03 μM. 16300944
Huh7 Function assay Functional activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50 = 0.22 μM. 16366601
Huh7 Function assay Effect on PPAR gamma transactivation activity in Huh7 cells, EC50 = 0.22 μM. 16451087
HEK293 Function assay Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay 16680159
HEK293 Function assay Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay 16680159
CV1 Function assay Transactivation of PPARgamma in CV1 cells, EC50 = 0.076 μM. 16821769
NIH3T3 Function assay Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay, EC50 = 0.32 μM. 16854085
CV1 Function assay Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay, EC50 = 0.308 μM. 16970391
HepG2 Function assay Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.158 μM. 16973358
HepG2 Function assay Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.158 μM. 16979341
CV1 Function assay Activity at human PPARgamma in CV1 cells, EC50 = 0.308 μM. 17005394
Huh7 Function assay Activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50 = 0.22 μM. 17034149
CV1 Function assay Agonist activity at PPARgamma in CV1 cells by transactivation assay, EC50 = 0.308 μM. 17129725
HepG2 Function assay Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.082 μM. 17157019
HEK293 Function assay Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay, EC50 = 0.035 μM. 17292606
HEK293 Function assay Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay, EC50 = 0.31 μM. 17343371
L6 Function assay Effect on fatty acid oxidation in rat L6 cells, EC50 = 5 μM. 17343371
HepG2/C3A Function assay Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay, EC50 = 0.0038 μM. 17403688
CV1 Function assay 24 hrs Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50 = 0.03 μM. 17507225
CV1 Function assay 24 hrs Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50 = 3.46 μM. 17507225
NIH3T3 Function assay Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay, EC50 = 0.32 μM. 17624777
HEK293 Function assay Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction, EC50 = 0.12 μM. 18029176
HEK293 Function assay Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay, EC50 = 0.19 μM. 18029176
CV1 Function assay Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay, EC50 = 0.308 μM. 18029178
HEK293 Function assay Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay, EC50 = 0.045 μM. 18291645
U2OS Function assay Agonist activity at human PPARgamma in U2OS cells by transactivation assay, EC50 = 0.02 μM. 18329751
HepG2 Function assay Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50 = 0.223 μM. 18394907
HepG2 Function assay Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control, EC50 = 0.05 μM. 18625559
RAW264.7 Function assay Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells, IC50 = 17.5 μM. 18809325
CV1 Function assay Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 0.033 μM. 18826205
CV1 Function assay Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 3.46 μM. 18826205
HepG2 Function assay Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50 = 0.039 μM. 18835719
HepG2 Function assay Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50 = 0.04 μM. 19053776
HeLa Function assay Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay, EC50 = 0.015 μM. 19275963
BL21 Function assay Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARgamma expressed in Escherichia coli BL21 cells by scintillation proximity assay, IC50 = 0.45 μM. 19349176
BHK21 Function assay Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay, EC50 = 0.45 μM. 19349176
COS1 Function assay 48 hrs Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay, EC50 = 0.02 μM. 19507861
COS1 Function assay Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay, EC50 = 0.02 μM. 19530681
U2OS Function assay Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay, EC50 = 0.05 μM. 19574056
MCF7 Function assay 0.1 uM 24 hrs Activation of human PPAR-gamma-dependent transcription expressed in human MCF7 cells assessed as induction of PPRE-reporter gene expression at 0.1 uM after 24 hrs by dual luciferase reporter gene assay relative to rosiglitazone 19719236
HepG2 Function assay Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay, EC50 = 0.039 μM. 19775169
HepG2 Function assay Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50 = 0.223 μM. 19783444
COS7 Function assay Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50 = 0.03 μM. 20138762
COS7 Function assay Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50 = 0.1 μM. 20138762
HEK Function assay Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay, EC50 = 0.035 μM. 20299214
HEK Function assay Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay, EC50 = 10.58 μM. 20299214
CHO-K1 Function assay Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay, EC50 = 0.1 μM. 20527969
3T3L1 Function assay 7 days Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in lipid accumulation after 7 days by Oil red O staining 20527969
HEK293T Function assay 1 uM 24 hrs Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay 21030263
CV1 Function assay Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50 = 0.1 μM. 21112784
HEK293 Function assay 16 to 20 hrs Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay, EC50 = 0.043 μM. 21128600
HepG2 Function assay 10 umol/L 24 hrs Increase in glucose consumption in human HepG2 cells at 10 umol/L after 24 hrs relative to control 21256748
HepG2 Function assay Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay, EC50 = 0.05 μM. 21450468
HepG2 Function assay Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay, EC50 = 0.01 μM. 21482446
CV1 Function assay 40 hrs Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay, EC50 = 0.1 μM. 21515063
3T3L1 Function assay 10 uM Increase in adiponectin mRNA levels in TNFalpha-induced mouse 3T3L1 cells pretreated at 10 uM before TNF-alpha challenge relative to control 21851089
COS7 Function assay Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50 = 0.043 μM. 21873070
Sf21 Function assay Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 6.4 μM. 21965623
Sf21 Function assay Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 40 μM. 21965623
COS-1 Function assay 24 hrs Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis, EC50 = 0.048 μM. 22051054
COS1 Function assay Binding affinity to human wild type PPARgamma LBD expressed in COS1 cells co-expressing GAL4 by scintillation proximity assay 22070604
HepG2 Function assay 20 hrs Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay, EC50 = 0.02 μM. 22081932
BL21 DE3 Function assay Displacement of [3H]rosiglitazone from N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells by scintillation proximity assay, Ki = 0.074 μM. 22081932
COS1 Function assay 24 hrs Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay, EC50 = 0.12 μM. 22197396
MG-63 Function assay Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay, EC50 = 0.011 μM. 22225641
293H DA Function assay 16 hrs Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay, EC50 = 0.0024 μM. 22582973
MG-63 Function assay 24 hrs Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay, EC50 = 0.011 μM. 22727448
Ac2F Function assay 0.1 to 10 uM 6 hrs Agonist activity at PPARgamma in rat Ac2F cells assessed as luciferase activity at 0.1 to 10 uM after 6 hrs by reporter gene assay 22819190
HepG2 Function assay Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay, EC50 = 0.1 μM. 22934537
THP1 Function assay 100 uM 3 hrs Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced MCP1 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control 22934537
THP1 Function assay 100 uM 3 hrs Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced IL6 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control 22934537
HepG2 Function assay 10 uM 24 hrs Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 0.1 uM of insulin 23025244
HepG2 Function assay 10 uM 24 hrs Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose 23025244
HepG2 Function assay 20 hrs Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.039 μM. 23171045
L02 Function assay 24 hrs Agonist activity at PPARgamma-LBD expressed in human L02 cells co-expressing pGL3-SV40-GAL4 after 24 hrs by luciferase reporter gene based transactivation assay, EC50 = 0.9 μM. 23186307
HEK293 Function assay 48 hrs Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50 = 43.71 μM. 23265844
HEK293 Function assay 10 uM Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells co-transfected with AP2-PPRE at 10 uM by luciferase reporter gene assay 23273519
HEK293 Function assay Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay, EC50 = 0.004 μM. 23286787
HEK293 Function assay 24 hrs Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.1 μM. 23294830
CMT93 Function assay 10 uM 30 mins Induction of PPAR-gamma promoter activity in LPS-stimulated mouse CMT93 cells at 10 uM preincubated for 30 mins before LPS-challenge measured after 6 hrs post challenge by luciferase reporter gene assay 23416190
HepG2 Function assay Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50 = 0.002 μM. 23502212
HepG2 Function assay Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50 = 0.01 μM. 23502212
L6 Function assay 24 hrs Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin, EC50 = 4.49 μM. 23992862
L6 Function assay 16 hrs Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis, IC50 = 4.8 μM. 24813738
HEK293 Function assay 10 uM 24 hrs Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay 24890090
HEK293 Function assay 24 hrs Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50 = 0.03 μM. 24955889
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 16 μM. 24996143
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 20.3 μM. 24996143
MDA-MB-231 Growth inhibition assay 24 hrs Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 5.23 μM. 25278236
HEK293 Function assay Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.01 μM. 25305688
HepG2 Function assay 20 hrs Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay, EC50 = 1.6 μM. 25437304
HEK293 Function assay 24 hrs Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter gene assay 25442322
HepG2 Function assay Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay, EC50 = 0.039 μM. 25462281
HepG2 Function assay 20 hrs Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay, EC50 = 0.04 μM. 25497132
HepaR Function assay 1 uM 1 day Agonist activity at PPARgamma in human HepaR cells assessed as increase in FABP1 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control 25497132
HepaR Function assay 1 uM 1 day Agonist activity at PPARgamma in human HepaR cells assessed as increase in ANGPTL4 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control 25497132
HepaR Function assay 1 uM 1 day Agonist activity at PPARgamma in human HepaR cells assessed as increase in HMGCS2 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control 25497132
C2C12 Function assay 30 uM 2 hrs Induction of 2-deoxy-[3H]-glucose uptake in mouse C2C12 cells at 30 uM after 2 hrs by liquid scintillation counting analysis 25835537
MCF7 Function assay 16 hrs Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay, EC50 = 0.087 μM. 26226490
HEK293 Function assay 10 uM 24 hrs Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM incubated for 24 hrs by luciferase reporter gene assay 26384286
3T3L1 Function assay 2 uM Transactivation of PPARgamma in mouse 3T3L1 cells assessed as adipocyte differentiation by measuring lipid accumulation at 2 uM by Oil Red O staining-based assay 26595749
3T3L1 Function assay 2 uM Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in FABP4 expression at 2 uM by qPCR method 26595749
3T3L1 Function assay 2 uM Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in GTUT4 expression at 2 uM by qPCR method 26595749
3T3L1 Function assay 2 uM Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin expression at 2 uM by qPCR method 26595749
3T3L1 Function assay 2 uM Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in LPL expression at 2 uM by qPCR method 26595749
HEK293 Function assay 1 uM 24 hrs Agonist activity at PPAR gamma (unknown origin) transfected in HEK293 cells at 1 uM after 24 hrs by dual-luciferase reporter gene assay 26988304
C2C12 Function assay 20 uM 4 hrs Transactivation of PPARgamma in mouse C2C12 cells assessed as increase in GLUT-4 mediated 2-NBDG uptake at 20 uM at 4 hrs by fluorescence assay 27100993
HEK293 Function assay 24 hrs Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.26 μM. 27591006
HepG2 Function assay 20 hrs Transactivation of GAL4-fused human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.04 μM. 28076827
HT-29 Function assay 10 uM 24 hrs Agonist activity at PPARgamma in human HT-29 cells harboring APC mutant assessed as inhibition of Wnt/beta-catenin signaling pathway by measuring decrease in CyclinD1 level at 10 uM treated for 24 hrs by Western blot method 28076827
COS7 Function assay 24 hrs Transactivation of human Gal4-fused PPARgamma LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.004 μM. 28609708
COS7 Function assay 24 hrs Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 10 μM. 28609708
HEK293 Function assay 18 hrs Agonist activity at GAL4-fused PPARgamma LBD (unknown origin) expressed in HEK293 cells assessed as receptor transactivation after 18 hrs by dual luciferase reporter gene assay, EC50 = 0.04 μM. 28667876
Ac2F Function assay 5 uM 6 hrs Agonist activity at full length human flag-tagged PPARgamma1 LBD expressed in rat Ac2F cells coexpressing PPRE-X3-TK at 5 uM after 6 hrs by one-glo luciferase reporter gene assay 29389121
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
3T3-L1 Function assay 1 uM 15 days Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase in CD36 mRNA expression at 1 uM after 15 days by quantitative real-time PCR method 29878767
3T3-L1 Function assay 1 uM 15 days Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as induction of adipocyte differentiation at 1 uM after 15 days by Oil Red O staining-based assay 29878767
3T3-L1 Function assay 1 uM 15 days Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase in CPT1A mRNA expression at 1 uM after 15 days by quantitative real-time PCR method 29878767
HepG2 Function assay 20 hrs Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.039 μM. 30199253
3T3L1 Function assay 5 uM Induction of lipid accumulation in mouse 3T3L1 cells at 5 uM by Oil Red O staining-based assay 30199253
3T3L1 Function assay 2 uM Induction of lipid accumulation in mouse 3T3L1 cells at 2 uM by Oil Red O staining-based assay 30199253
HepG2 Function assay >100 nM 20 hrs Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at >100 nM after 20 hrs in presence of 5 uM PPARgamma antagonist GW9662 by luciferase reporter gene assay 30199253
COS7 Function assay 24 hrs Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.396 μM. 30220602
COS7 Function assay 24 hrs Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.396 μM. 30241907
HEK293 Function assay 18 hrs Agonist activity at human GAL4 fused PPARgamma-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay, EC50 = 0.12 μM. 30296685
HEL 293H Function assay 16 hrs Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay, EC50 = 0.008 μM. 30429097
HEK293 Function assay 18 hrs Transactivation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay, EC50 = 0.039 μM. ChEMBL
CV-1 Function assay Tested for transactivation of human PPAR gamma-Gal4 chimera in CV-1 cells, EC50 = 0.05 μM. ChEMBL
3T3L1 Function assay 7 days Upregulation of FAS protein expression in differentiated mouse 3T3L1 cells after 7 days by western blot analysis ChEMBL
3T3L1 Function assay 7 days Upregulation of aP2 protein expression in differentiated mouse 3T3L1 cells after 7 days by western blot analysis ChEMBL
3T3L1 Function assay 24 hrs Inhibition of chronic insulin-stimulated insulin resistance in differentiated mouse 3T3L1 cells assessed as 2-deoxy-D-[3H]-glucose uptake after 24 hrs by scintillation counting analysis ChEMBL
3T3L1 Function assay 10 uM 24 hrs Induction of insulin-stimulated 2-deoxy-D-[3H]-glucose uptake in differentiated mouse 3T3L1 cells at 10 uM after 24 hrs by scintillation counting analysis ChEMBL
3T3L1 Function assay 2 uM 14 days Agonist activity at PPAR in mouse 3T3L1 cells assessed as increase in adipocyte differentiation at 2 uM after 14 days by Oil Red O staining method ChEMBL
U2OS Function assay 10 uM 24 hrs Activation of PPARG (unknown origin) expressed in human U2OS cells at 10 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
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Solubility

In vitro
Batch:

DMSO : 71 mg/mL (198.64 mM)
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Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 357.43 Formula

C18H19N3O3S

 Storage (From the date of receipt)
CAS No. 122320-73-4 Download SDF Storage of Stock Solutions

Synonyms BRL 49653 Smiles CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3

Mechanism of Action

Targets/IC50/Ki
PPAR
(Cell-free assay)
TRPC
Ferroptosis
In vitro

Rosiglitazone markedly increase phosphorylation of threonine 172 within the α subunit of AMPK, with increased AMP:ATP ratio. This compound has been reported to decrease cholesterol synthesis in a number of cell lines in a peroxisome proliferator-activated receptor γ-independent manner. It activates both α1- and α2-containing AMPK complexes, and this leads to a marked increase in the phosphorylation of acetyl-CoA carboxylase.

This chemical activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro.

It increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected.

This compound changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes.

In vivo

Rosiglitazone administration results in significant bone loss, including a decrease in bone volume, trabecular width, and trabecular number and an increase in trabecular spacing. This compound also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. It decreases the expression of the osteoblast-specific genes Runx2/Cbfa1, Dlx5, and alpha1(I)collagen, whereas the expression of the adipocyte-specific fatty acid binding protein aP2 is increased.

This chemical upregulates gene transcripts encoding mitochondrial proteins in white adipocytes from ob/ob mice accompanied by an increase in mitochondrial mass and changes in mitochondrial structure.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/15520860/
  • [5] https://pubmed.ncbi.nlm.nih.gov/21406603/
  • [6] https://pubmed.ncbi.nlm.nih.gov/30737476/
  • [7] https://pubmed.ncbi.nlm.nih.gov/35131600/
  • [8] https://pubmed.ncbi.nlm.nih.gov/28892640/

Applications

Methods Biomarkers Images PMID
Western blot Cyclin D1 / CDK2 / CDK4 / Bax / Bcl-2
S2556-WB1
29725405
Immunofluorescence PPARγ / E-cadherin
S2556-IF1
27145370
Growth inhibition assay Cell viability
S2556-viability1
29725405

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02737709 Terminated
Non-small Cell Lung Cancer
Sun Yat-sen University
 March 2016 Phase 2
NCT01402076 Completed
Healthy Volunteers
Vanda Pharmaceuticals
 August 2011 Phase 1
NCT01100619 Completed
Papillary Thyroid Cancer|Follicular Thyroid Cancer|Huerthle Cell Thyroid Cancer|Renal Cell Carcinoma
Exelixis
 April 2010 Phase 1
NCT01415128 Completed
Erectile Dysfunction
VIVUS LLC
 April 2010 Phase 1
NCT01376063 Completed
Healthy Adult Subjects
FibroGen
 March 2010 Phase 1

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