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T0901317 Liver X Receptor agonist

Name: T0901317
SKU: S7076
Availability: InStock
Rating: 5 (23 reviews)

Cat.No.S7076

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of 20nM for LXRα and 5 μM for FXR, respectively. This compound is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. It significantly suppresses cell proliferation and induces apoptosis.

Chemical Structure

Molecular Weight: 481.33

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS
Related Products	GW3965 Hydrochloride LXR-623 SR9243 AZ876 Abequolixron (RGX-104) Desmosterol GSK3987 GSK2033 LXRα Antibody [C12J22]

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
THP1 cells	Function assay		Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL, EC50=3 nM
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
CHO cells	Function assay		Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay, EC50=16 nM
HEK293 cells	Function assay		Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation, EC50=19 nM
mouse J774 cells	Function assay		Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression, EC50=0.027 μM
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
HuH7 cells	Function assay		Upregulation of SREB1c mRNA level in human HuH7 cells, EC50=0.036 μM
HepG2 cells	Function assay		Effect on SREBP1c gene expression in human HepG2 cells, EC50=0.061 μM
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
CV1 cells	Function assay		Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay, EC50=0.14 μM
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	481.33	Formula	C₁₇H₁₂F₉NO₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	293754-55-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (199.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 96 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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.

Mechanism of Action

Targets/IC₅₀/Ki	LXR ^[1] (Cell reporter assay) 50 nM(EC50) FXR ^[2] 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. This compound upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism.^[1] It 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] This chemical is also a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). It binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. This compound induces expression not only of LXR target genes, but also of PXR target genes in cells and animals, including the scavenger receptor CD36. ^[3] It decreases amyloid-β production in primary neurons in vitro. ^[4] This chemical 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. It 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]
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, this compound causes a statistically significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain these mice. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/10968783/ [2] https://pubmed.ncbi.nlm.nih.gov/15464433/ [3] https://pubmed.ncbi.nlm.nih.gov/17418145/ [4] https://pubmed.ncbi.nlm.nih.gov/15557325/ [5] https://pubmed.ncbi.nlm.nih.gov/19887649/ [6] https://pubmed.ncbi.nlm.nih.gov/35169231/

Applications

Methods	Biomarkers	Images	PMID
Western blot	LXR-β / LXR-α EGFR / p-PI3K p55 / p-PI3K p85 / PI3K p85 / p-PDK1 / PDK1		28097086

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