1. Metabolic Enzyme/Protease
    Autophagy
  2. FXR
    Autophagy
  3. Cilofexor

Cilofexor (Synonyms: GS-9674)

Cat. No.: HY-109083 Purity: 99.82%
Handling Instructions

Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.

For research use only. We do not sell to patients.

Cilofexor Chemical Structure

Cilofexor Chemical Structure

CAS No. : 1418274-28-8

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 194 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
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10 mg USD 240 In-stock
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25 mg USD 490 In-stock
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50 mg USD 840 In-stock
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100 mg USD 1400 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research[1][2].

IC50 & Target

EC50: 43 nM (FXR)[1]

In Vivo

Cilofexor (GS-9674; 30 mg/kg; oral gavage; once daily; for 10 weeks; male Wistar rats) treatment significantly increases Fgf15 expression in the ileum and decreased Cyp7a1 in the liver in nonalcoholic steatohepatitis (NASH) rats. Liver fibrosis and hepatic collagen expression are significantly reduced. Cilofexor also significantly reduces hepatic stellate cell (HSC) activation and significantly decreases portal pressure, without affecting systemic hemodynamics[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats received a choline-deficient high fat diet (CDHFD)[3]
Dosage: 30 mg/kg
Administration: Oral gavage; once daily; for 10 weeks
Result: Significantly increased Fgf15 expression in the ileum and decreased Cyp7a1 in the liver. Liver fibrosis and hepatic collagen expression were significantly reduced.
Clinical Trial
Molecular Weight

586.85

Formula

C₂₈H₂₂Cl₃N₃O₅

CAS No.

1418274-28-8

SMILES

ClC1=C(C2(CN(C3=CC(C(O)=O)=CC=N3)C2)O)C=CC(OCC4=C(C5CC5)ON=C4C(C(Cl)=CC=C6)=C6Cl)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (85.20 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7040 mL 8.5201 mL 17.0401 mL
5 mM 0.3408 mL 1.7040 mL 3.4080 mL
10 mM 0.1704 mL 0.8520 mL 1.7040 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.82%

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Keywords:

CilofexorGS-9674GS9674GS 9674FXRAutophagyNR1H4PSCnonsteroidalsafetyanti-inflammatoryantifibroticNASHoralInhibitorinhibitorinhibit

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Cilofexor
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HY-109083
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