T0901317

Catalog No.S7076

T0901317 Chemical Structure

Molecular Weight(MW): 481.33

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively.

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USD 470 In stock
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Cited by 4 Publications

3 Customer Reviews

  • (C) Cells were pretreated with DMSO or T0901317 (5 μM), then incubated with 100 mg/L ox-LDL for 6 h.

    FEBS Lett, 2015, 589(1):52-8. . T0901317 purchased from Selleck.

    THP-1 macrophages were pretreated with 5 μg/mL T0901317 for 30 min and incubated with 100 μmol/L Hcy for 24 h. protein levels were determined.

    Life Sci, 2018, doi:10.1016/j.lfs.2018.10.060. T0901317 purchased from Selleck.

  • a Entrapment and loading efficiencies of T0901317- liposomes and anti-ICAM-1-T0901317- liposomes at two lipid to T0901317 weight ratios (5:1 and 10:1). b In vitro drug release of T0901317- liposomes (squares) and anti-ICAM-1-T0901317- liposomes (circles) at different time points. Values are expressed as the means ± SD (n = 3)

    Nanoscale Res Lett, 2017, 12(1):322. T0901317 purchased from Selleck.

Purity & Quality Control

Choose Selective Liver X Receptor Inhibitors

Biological Activity

Description T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively.
Targets
LXR [1]
(Cell reporter assay)
FXR [2]
50 nM(EC50) 5 μM(EC50)
In vitro

T0901317 acts through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. T0901317 upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism.[1] T0901317 displays an EC50 of ~ 5 μM for activation of bile acid farnesoid X receptors (FXRs), 10-fold more potent than natural FXR ligand chenodeoxycholic acid. [2] T0901317, is also a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 induces expression not only of LXR target genes, but also of PXR target genes in cells and animals, including the scavenger receptor CD36. [3] T0901317 decreases amyloid-β production in primary neurons in vitro. [4] T0901317 is found to directly bind to RORα and RORγ with high affinity (Ki = 132 and 51 nM, respectively), resulting in the modulation of the receptor's ability to interact with transcriptional cofactor proteins. T0901317 represses RORα/γ-dependent transactivation of ROR-responsive reporter genes and in HepG2 cells reduces recruitment of steroid receptor coactivator-2 by RORα at an endogenous ROR target gene (G6Pase). [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 cells NGHyPVBHfW6ldHnvckBie3OjeR?= NUK3VIVZW3SrbYXsZZRqd25ib3[gX|NJZWOqb3zld5Rmem:uIHXm[ox2gCCrbjDoeY1idiCWSGCxJIZw[W1iY3XscJMhdG:jZHXkJJdqfGhiYXOtUGRNNCCHQ{WwQVMhdk1? NFnUWlEyQTl4Mki5Ni=>
COS7 cells MlTkSpVv[3Srb36gZZN{[Xl? NVizSXZ4OTZiaB?= MkjMRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDMXHJj\XSjIILlZ4VxfG:{IITyZY5{\mWldHXkJIlvKEORU{egZ4VtdHNiYX\0[ZIhOTZiaILzJIJ6KHKncH;yeIVzKHS{YX7zZYN1cX[jdHnvckBie3OjeTygSWM2OD1zMTDuUS=> MnXYNVc2QDd3N{O=
CHO cells NFvNOHNHfW6ldHnvckBie3OjeR?= M3;HfGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhTKGKndHGgdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTDy[ZBwenSncjDhd5NigSxiRVO1NF0yPiCwTR?= NWnqOZhUOTl6NUO0OlI>
HEK293 cells MX\GeY5kfGmxbjDhd5NigQ>? M3XkNmFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgS4FtPCC2cnHud4FkfGm4YYTpc44tKEWFNUC9NVkhdk1? M1\pTlIxOzVyMEC1
mouse J774 cells M2GxUWZ2dmO2aX;uJIF{e2G7 M{HTXmFod26rc4SgZYN1cX[rdImgZZQhVFiUYnX0ZUBqdiCvb4Xz[UBLPzd2IHPlcIx{KGG|c3Xzd4VlKGG|IIXwdoVofWyjdHnvckBw\iCDQlPBNUBuWk6DIHX4dJJme3Orb36sJGVEPTB;MD6wNlch|ryP NGjo[GQyQTh3M{S2Ni=>
mouse J774A1 cells Mn\FSpVv[3Srb36gZZN{[Xl? MoXUNVghcA>? MV;JcoR2[3Srb36gc4YhSUKFQUGgcXJPSSCneIDy[ZN{cW:wIHnuJI1wfXOnIFq3O|RCOSClZXzsd{Bi\nSncjCxPEBpenNiYomgVnQuWEOULDDFR|UxRTBuMEO0JO69VQ>? NFXWOWgyQTN7NEizNi=>
HuH7 cells NUfhW2lGTnWwY4Tpc44h[XO|YYm= NXy3c3dlXXC{ZXf1cIF1cW:wIH;mJHNTTUJzYzDtVm5CKGyndnXsJIlvKGi3bXHuJGh2UDdiY3XscJMtKEWFNUC9NE4xOzZizszN MnPUNlA{QDJyMUm=
HepG2 cells NHfSO|NHfW6ldHnvckBie3OjeR?= M2PiUWVn\mWldDDvckBUWkWEUEHjJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{whTUN3ME2wMlA3OSEQvF2= M2izcVE5QTd|Mki4
SH-SY5Y cells MmrmSpVv[3Srb36gZZN{[Xl? NHG1epczPCCq M1HVT2Fod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDlfJBz\XO|ZXSgbY4hcHWvYX6gV2guW1l3WTDj[YxteyClbz30doFve2[nY4Tl[EB4cXSqIFfhcFQuVEKGIHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6wO|Uh|ryP MYWxPVI3PDR6MR?=
CV1 cells NWTXcVRKTnWwY4Tpc44h[XO|YYm= M4izR3Rz[W6|YXP0bZZifGmxbjDv[kBNYFKkZYThJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKEOYMTDj[YxteyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NE4yPCEQvF2= MVeyOVQ{PTF3MR?=
human H4 cells Mn;RSpVv[3Srb36gZZN{[Xl? MWXF[oZm[3Rib36g[4FudWFvc3XjdoV1[XOnIHHjeIl3cXS7IHnuJIh2dWGwIFi0JINmdGy|IHX4dJJme3OrbnegRXBRPjl3IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKEGveXzvbYQh[mW2YT20NkBnd3KvYYTpc44hVFCHQ1ygZZN{[XluIFXDOVA:Oy54IN88US=> M2LCZ|E4PzJ|Mkm4

... Click to View More Cell Line Experimental Data

In vivo T0901317 treatment of 11-week-old APP23 mice for 6 days shows a significant increase in ABCA1 expression and a decrease in the ratio of soluble APP (sAPP)β- to sAPPα-cleavage products. Most importantly, the treatment causes a statistically significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain these mice. [4]

Protocol

Animal Research:

[4]

+ Expand
  • Animal Models: APP23 mice
  • Formulation: propylene glycol/Tween 80 (4/1)
  • Dosages: 50 mg/kg/day
  • Administration: gastric gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (199.44 mM)
Ethanol 96 mg/mL (199.44 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+35% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
6mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 481.33
Formula

C17H12F9NO3S

CAS No. 293754-55-9
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID