T0901317

Catalog No.S7076

For research use only.

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively. T0901317 is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. T0901317 significantly suppresses cell proliferation and induces apoptosis.

T0901317 Chemical Structure

CAS No. 293754-55-9

Selleck's T0901317 has been cited by 14 publications

Purity & Quality Control

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Biological Activity

Description T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively. T0901317 is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. T0901317 significantly suppresses cell proliferation and induces apoptosis.
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 MoK3SpVv[3Srb36gZZN{[Xl? Mor0V5RqdXWuYYTpc44hd2ZiW{PIYYNpd2ync4Tldo9tKGWoZnz1fEBqdiCqdX3hckBVUFBzIH\vZY0h[2WubIOgcI9i\GWmIIfpeIgh[WNvTFTMMEBGSzVyPUOgcm0> M4K5NlE6QTZ{OEmy
COS7 cells NXGzS4s3TnWwY4Tpc44h[XO|YYm= M2rpNlE3KGh? M2XufGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDy[YNmeHSxcjD0doFve2[nY4Tl[EBqdiCFT2O3JINmdGy|IHHmeIVzKDF4IHjyd{BjgSC{ZYDvdpRmeiC2cnHud4FkfGm4YYTpc44h[XO|YYmsJGVEPTB;MUGgcm0> NF7lcWIyPzV6N{W3Ny=>
CHO cells NF\abo5HfW6ldHnvckBie3OjeR?= MX3B[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFzYVkBj\XSjIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nlicnXwc5J1\XJiYYPzZZktKEWFNUC9NVYhdk1? MW[xPVg2OzR4Mh?=
HEK293 cells NXraWZpMTnWwY4Tpc44h[XO|YYm= M1fw[GFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgS4FtPCC2cnHud4FkfGm4YYTpc44tKEWFNUC9NVkhdk1? NFrLRWEzODN3MECwOS=>
mouse J774 cells NITQb4RHfW6ldHnvckBie3OjeR?= NEjSOGVC\2:waYP0JIFkfGm4aYT5JIF1KEy[UnLleIEhcW5ibX;1d4UhUjd5NDDj[YxteyCjc4Pld5Nm\CCjczD1dJJm\3WuYYTpc44hd2ZiQVLDRVEhdVKQQTDlfJBz\XO|aX;uMEBGSzVyPUCuNFI4KM7:TR?= NUXieWI6OTl6NUO0OlI>
mouse J774A1 cells M17BTGZ2dmO2aX;uJIF{e2G7 MX2xPEBp M1j2bmlv\HWldHnvckBw\iCDQlPBNUBuWk6DIHX4dJJme3Orb36gbY4hdW:3c3WgTlc4PEFzIHPlcIx{KGGodHXyJFE5KGi{czDifUBTXC2SQ2KsJGVEPTB;MDywN|Qh|ryP M{XL[|E6Ozl2OEOy
HuH7 cells MUPGeY5kfGmxbjDhd5NigQ>? MVXVdJJm\3WuYYTpc44hd2ZiU2LFRlFkKG2UTlGgcIV3\WxiaX6gbJVu[W5iSIXIO{Bk\WyuczygSWM2OD1yLkCzOkDPxE1? MVeyNFM5OjBzOR?=
HepG2 cells M3;wN2Z2dmO2aX;uJIF{e2G7 NFXMd3pG\m[nY4Sgc44hW1KHQmCxZ{Bo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMtKEWFNUC9NE4xPjFizszN Ml3qNVg6PzN{OEi=
SH-SY5Y cells M3POZmZ2dmO2aX;uJIF{e2G7 M1ntOFI1KGh? NVz5[HQ2SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFKkZYThJIV5eHKnc4Pl[EBqdiCqdX3hckBUUC2VWUXZJINmdGy|IHPvMZRz[W6|ZnXjeIVlKHerdHigS4FtPC2OQlSgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlA4PSEQvF2= MmnUNVkzPjR2OEG=
CV1 cells MXrGeY5kfGmxbjDhd5NigQ>? MXHUdoFve2GldHn2ZZRqd25ib3[gUHhT[mW2YTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBEXjFiY3XscJMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuNVQh|ryP M3nMUFI2PDN3MUWx
human H4 cells MoLCSpVv[3Srb36gZZN{[Xl? NWjI[XByTW[oZXP0JI9vKGejbX3hMZNm[3KndHHz[UBi[3Srdnn0fUBqdiCqdX3hckBJPCClZXzsd{BmgHC{ZYPzbY5oKEGSUE[5OUBie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDBcZltd2mmIHLleIEuPDJiZn;ycYF1cW:wIFzQSWNNKGG|c3H5MEBGSzVyPUOuOkDPxE1? MmXWNVc4OjN{OUi=
Assay
Methods Test Index PMID
Western blot LXR-β / LXR-α ; EGFR / p-PI3K p55 / p-PI3K p85 / PI3K p85 / p-PDK1 / PDK1 28097086
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 (from reference)

Animal Research:

[4]

  • Animal Models: APP23 mice
  • Dosages: 50 mg/kg/day
  • Administration: gastric gavage

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 481.33
Formula

C17H12F9NO3S

CAS No. 293754-55-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)S(=O)(=O)N(CC(F)(F)F)C2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

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.

Handling Instructions

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