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Cilofexor (GS-9674) FXR agonist

Name: Cilofexor (GS-9674)
Brand: Selleck Chemicals
SKU: S6547
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S6547

Cilofexor(GS-9674) is a potent, selective oral agonist of farnesoid X receptor (FXR) with an EC50 of 43 nM. It has demonstrated anti-inflammatory, antifibrotic effects, and reduced portal pressure in preclinical liver fibrosis models, showing potential therapeutic benefit for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.

Chemical Structure

Molecular Weight: 586.85

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Quality Control

Batch: S654701 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.45%

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS/MSDS
Datasheet

99.45

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other FXR Inhibitors	GW4064 Guggulsterone E&Z Turofexorate Isopropyl (XL335) fexaramine BAR502 Nidufexor (LMB-763) Tropifexor (LJN452) Mebhydroline Vonafexor (EYP001) DY268

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (170.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
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.	0.500mg/ml (0.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Chemical Information, Storage & Stability

Molecular Weight	586.85	Formula	C₂₈H₂₂Cl₃N₃O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1418274-28-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GS-9674			SMILES	C1CC1C2=C(C(=NO2)C3=C(C=CC=C3Cl)Cl)COC4=CC(=C(C=C4)C5(CN(C5)C6=NC=CC(=C6)C(=O)O)O)Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	FXR 43 nM(EC50)
References	[1] https://pubmed.ncbi.nlm.nih.gov/30661255/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-11-26)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04971785	COMPLETED	Nonalcoholic Steatohepatitis	Gilead Sciences	2021-08-09	PHASE2
NCT03890120	TERMINATED	Primary Sclerosing Cholangitis	Gilead Sciences	2019-03-27	PHASE3
NCT04060147	TERMINATED	Primary Sclerosing Cholangitis; Compensated Cirrhosis	Gilead Sciences	2019-10-17	PHASE1
NCT03987074	COMPLETED	Nonalcoholic Steatohepatitis	Gilead Sciences	2019-07-29	PHASE2
NCT03449446	COMPLETED	Nonalcoholic Steatohepatitis	Gilead Sciences	2018-03-21	PHASE2
NCT02943447	TERMINATED	Primary Biliary Cholangitis	Gilead Sciences	2016-12-01	PHASE2

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