Home Metabolism Liver X Receptor agonist - FXR agonist - ROR agonist - Apoptosis related activator T0901317 For research use only.

T0901317

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of 20nM for LXRα and 5 μM for FXR, 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

T0901317 Chemical Structure

CAS No. 293754-55-9

Purity & Quality Control

T0901317 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 cells Function assay Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL, EC50=3 nM 19962892
COS7 cells Function assay 16 h Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay, EC50=11 nM 17587573
CHO cells Function assay Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay, EC50=16 nM 19853462
HEK293 cells Function assay Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation, EC50=19 nM 20350005
mouse J774 cells Function assay Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression, EC50=0.027 μM 19853462
mouse J774A1 cells Function assay 18 h Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR, EC50=0,034 μM 19394832
HuH7 cells Function assay Upregulation of SREB1c mRNA level in human HuH7 cells, EC50=0.036 μM 20382019
HepG2 cells Function assay Effect on SREBP1c gene expression in human HepG2 cells, EC50=0.061 μM 18973288
SH-SY5Y cells Function assay 24 h Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay, EC50=0.075 μM 19264481
CV1 cells Function assay Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay, EC50=0.14 μM 25435151
human H4 cells Function assay Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay, EC50=3.6 μM 17723298
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Biological Activity

Description T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of 20nM for LXRα and 5 μM for FXR, 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
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 Research Cell lines BMDMs
Concentrations 5 µM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of drug for 24 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot LXR-β / LXR-α EGFR / p-PI3K p55 / p-PI3K p85 / PI3K p85 / p-PDK1 / PDK1 28097086
In Vivo
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]
Animal Research Animal Models APP23 mice
Dosages 50 mg/kg/day
Administration gastric gavage

Chemical Information & Solubility

Molecular Weight 481.33 Formula

C17H12F9NO3S
CAS No. 293754-55-9 SDF Download T0901317 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 96 mg/mL ( (199.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 96 mg/mL

Water : Insoluble


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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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