Pioglitazone HCl

Synonyms: AD-4833, U-72107E

Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.

Pioglitazone HCl Chemical Structure

Pioglitazone HCl Chemical Structure

CAS: 112529-15-4

Selleck's Pioglitazone HCl has been cited by 10 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.88%
99.88

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS cells Function assay Transcriptional activation in COS cells expressing PPAR gamma and RXR alpha; values in the parentheses indicates 95% confidence interval, EC50=0.49 μM 11906293
HepG2 cells Function assay Peroxisome proliferator activated receptor gamma agonistic activity in HepG2 cells, EC50=7.6 μM 10714503
CV-1 Function assay In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50=0.69μM. 8576907
3T3-L1 Function assay Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.16μM. 9599241
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=0.58884μM. 9836620
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=0.58μM. 11720854
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=0.55μM. 16821769
Cos7 Function assay 14 hrs Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay, EC50=0.3μM. 20307981
3T3L1 Function assay 100 umol/L Increase in PPARgamma mRNA levels in mouse 3T3L1 cells at 100 umol/L by RT-PCR 20392645
CHO Function assay Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay, EC50=0.14μM. 20656494
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
COS-1 Function assay Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50=0.39μM. 21130649
CHO Function assay 24 hrs Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay, EC50=0.39μM. 21377875
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=0.3μM. 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=0.3μM. 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=2μM. 21965623
HepG2 Function assay 20 hrs Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay, EC50=0.57μM. 22341573
HEK293 Function assay 18 hrs Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay, EC50=0.8μM. 23102891
COS7 Function assay Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay, EC50=0.2μM. 23130964
THP1 Antiinflammatory assay 1 hr Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA, IC50=18.84μM. 23811092
THP1 Antiinflammatory assay 2 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA, IC50=18.6μM. 24531227
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 18 hrs Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay, EC50=0.21μM. 25333853
COS7 Function assay Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay, EC50=0.2μM. 26595749
THP1 Function assay 10 uM 24 hrs Upregulation of ABCA1 mRNA expression in human THP1 cells at 10 uM after 24 hrs by qPCR method relative to control 27220065
THP1 Function assay 10 uM 24 hrs Upregulation of ABCG1 mRNA expression in human THP1 cells at 10 uM after 24 hrs by qPCR method relative to control 27220065
COS7 Function assay 42 hrs Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay, EC50=0.5μM. 27560282
COS7 Function assay 42 hrs Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay, EC50=0.32μM. 27569195
COS7 Function assay 42 hrs Transactivation of Gal4 fused human PPARgamma LBD expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay, EC50=0.38μM. 27918994
PC3 Function assay 50 uM 24 hrs Increase in p21(WAF1) protein expression in human PC3 cells at 50 uM incubated for 24 hrs by Western blot analysis 28395220
MDA-MB-231 Function assay 50 uM 24 hrs Increase in p21(WAF1) protein expression in human MDA-MB-231 cells at 50 uM incubated for 24 hrs by Western blot analysis 28395220
HEK293 Function assay 24 hrs Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50=1.1μM. 28465099
HEK293 Function assay 4 hrs Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay, IC50=22μM. 28465099
SCC15 Cytotoxicity assay 50 uM 24 hrs Cytotoxicity against human SCC15 cells transfected with PPARalpha siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay 29031063
SCC15 Cytotoxicity assay 50 uM 24 hrs Cytotoxicity against human SCC15 cells transfected with PPARbeta siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay 29031063
HepG2 Function assay 24 hrs Agonist activity at PPARgamma in human HepG2 cells assessed as activation of PPRE incubated for 24 hrs by dual luciferase reporter gene assay, EC50=0.24μM. 30001846
HEK293BENA Function assay 24 hrs Transactivation of GAL4-fused human PPARgamma transfected in HEK293BENA cells after 24 hrs by steady glo-luciferase reporter gene assay, EC50=2.053μM. 30351933
HEK293 Function assay 18 hrs Transactivation of human full length PPARgamma expressed in HEK293 cells after 18 hrs by luciferase reporter gene based luminescence assay, EC50=0.1μM. 30362739
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=0.098μM. 30429097
3T3L1 Function assay 10 uM 24 hrs Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in AP1 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis 30594432
3T3L1 Function assay 10 uM 24 hrs Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in CD36 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis 30594432
3T3L1 Function assay 10 uM 24 hrs Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in Glut4 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis 30594432
3T3L1 Function assay 10 uM 24 hrs Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis 30594432
stem cells Function assay 5 days Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in adiponectin production measured on day 5 in presence of IDX by ELISA, EC50=0.35μM. 30672698
HEK293T Function assay 18 hrs Transactivation of full length human PPARgamma2 expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay, EC50=0.25μM. 30676741
HEK293T Function assay 18 hrs Transactivation of chimeric Gal4 yeast DBD fused-PPARgamma LBD (unknown origin) expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay, EC50=0.35μM. 30676741
HepG2 Function assay 30 uM Binding affinity to NAF1 (unknown origin) expressed in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM 30770154
HepG2 Function assay 30 uM Binding affinity to NAF1 in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM 30770154
COS7 Function assay 39 hrs Transactivation of Gal4-fused human PPARgamma transfected in COS7 cells co-transfected with pGAL5-TK-pGL3 and pRennilla-CMV incubated for 39 hrs by dual luciferase reporter assay, EC50=1.4μM. 31648125
K562 Function assay 10 uM 72 hrs Induction of sensitization to imatinib-induced cytotoxicity in imatinib-resistant human K562-IMA[r] cells assessed as induction of cell death at 10 uM after 72 hrs in presence of 1 uM imatinib by propidium iodide/Triton-X100 dye based FACS analysis 31648125
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Biological Activity

Description Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
Targets
Ferroptosis [8] hPPARγ [1]
(Cell-free assay)
rPPARγ [6]
(Cell-free assay)
CYP2C8 [7]
(Cell-free assay)
CYP3A4 [7]
(Cell-free assay)
Click to View More Targets
0.93 μM(EC50) 0.99 μM(EC50) 1.7 μM(Ki) 11.8 μM(Ki)
In vitro
In vitro

Pioglitazone inhibits LPS-induced iNOS expression and NO generation, and inhibition of iNOS is sufficient to protect dopaminergic neurons against LPS insult. Pioglitazone protects dopaminergic neurons against LPS insult at least via inhibiting iNOS expression and NO generation, which is potentially mediated via inhibition of p38 MAPK activity. Pioglitazone inhibits LPS-induced phosphorylation of p38 MAPK. [1]

In Vivo
In vivo

Pioglitazone administered orally (0.3-3 mg/kg/d for 7 days) dose dependently reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in male fatty rats. Pioglitazone improves glucose tolerance and augmentes the glycemic response to exogenous insulin and clearance of plasma triglyceride in rats. [2] Pioglitazone-treated transgenic mice reveals improved muscle strength and body weight, exhibits a delayed disease onset, and survives significantly longer than nontreated SOD1-G93A mice. [3] Pioglitazone markedly decreases hyperglycemia, hyperlipidemia, hyperinsulinemia, and glucoseintolerance characterized as insulin resistant states in these rats and mice. Pioglitazone potentiates insulin-mediated glucose metabolism in the diaphragm and adipose tissues of yellow KK mice and enhanced the glycemic response to exogenous insulin in Zucker fatty rats. [4] Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of APPV717I transgenic mice. Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein levels in APPV717I transgenic mice. [5]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05946564 Not yet recruiting
ANCA Associated Vasculitis|Rapidly Progressive Glomerulonephritis|Crescentic Glomerulonephritis
Assistance Publique - Hôpitaux de Paris|Ministry of Health France
July 2023 Phase 3
NCT05305287 Recruiting
Non-Alcoholic Fatty Liver Disease|Type 2 Diabetes|Mitochondrial Metabolism Disorders
The University of Texas Health Science Center at San Antonio|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
November 1 2022 Phase 4
NCT05411965 Completed
Diabetes Mellitus Type 2
Boryung Pharmaceutical Co. Ltd
April 28 2022 Phase 1
NCT04501406 Recruiting
Type 2 Diabetes Mellitus (T2DM)|Nonalcoholic Steatohepatitis
University of Florida|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
December 15 2020 Phase 2
NCT04535700 Completed
Type 2 Diabetes
Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal
September 18 2020 Phase 4
NCT00904046 Recruiting
Uric Acid Kidney Stone Disease
University of Texas Southwestern Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Takeda Pharmaceuticals North America Inc.
September 5 2019 Not Applicable

Chemical Information & Solubility

Molecular Weight 392.9 Formula

C19H20N2O3S.HCl

CAS No. 112529-15-4 SDF Download Pioglitazone HCl SDF
Smiles CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (201.06 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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