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Chemical Structure| 1418274-28-8 Chemical Structure| 1418274-28-8

Structure of Cilofexor
CAS No.: 1418274-28-8

Chemical Structure| 1418274-28-8

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Cilofexor is a nonsteroidal FXR agonist. Cilofexor was well tolerated and led to significant improvements in liver biochemistries and markers of cholestasis in patients with primary sclerosing cholangitis in a 12-week study.

Synonyms: GS-9674

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Product Details of Cilofexor

CAS No. :1418274-28-8
Formula : C28H22Cl3N3O5
M.W : 586.85
SMILES Code : O=C(C1=CC(N2CC(O)(C3=CC=C(OCC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)C=C3Cl)C2)=NC=C1)O
Synonyms :
GS-9674
MDL No. :MFCD31731099
InChI Key :KZSKGLFYQAYZCO-UHFFFAOYSA-N
Pubchem ID :71228883

Safety of Cilofexor

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6JOlaHSD mice Cholestatic liver injury model Oral gavage 30 mg/kg Once daily for 3 weeks Cilofexor monotherapy and combination therapy with ASBTi ameliorated cholestatic liver injury, reduced plasma ALT and AST levels, and decreased liver inflammation and fibrosis markers. JHEP Rep. 2023 Sep 25;6(1):100917
Wistar rats NASH model Oral 10 mg/kg and 30 mg/kg Dose adjusted weekly, lasting for 6 weeks To evaluate the effect of Cilofexor on portal hypertension and hepatic fibrosis in NASH rats, results showed that Cilofexor significantly reduced portal pressure and hepatic fibrosis. Biomedicines. 2021 Jan 9;9(1):60
Mice Mdr2-/- mouse model Gavage 0, 10, 30, or 90 mg/kg Every 24 hours for 10 weeks To evaluate the anti-cholestatic, anti-inflammatory, and anti-fibrotic effects of cilofexor in the Mdr2-/- mouse model. Results showed that cilofexor improved serum biochemistry, reduced hepatic fibrosis, and decreased serum and intrahepatic bile acid levels. JHEP Rep. 2023 Aug 3;5(11):100874

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04060147 Primary Sclerosing Cholangitis... More >>|Compensated Cirrhosis Less << PHASE1 TERMINATED 2021-09-02 Arizona Liver Health, Chandler... More >>, Arizona, 85224, United States|California Liver Research Institute, Pasadena, California, 91105, United States|University of California San Francisco, Liver Clinic, San Francisco, California, 94143, United States|Schiff Center for Liver Diseases/University of Miami, Miami, Florida, 33136, United States|Piedmont Atlanta Hospital, Atlanta, Georgia, 30309, United States|Indiana University Health University Hospital, Indianapolis, Indiana, 46202, United States|Louisiana Research Center, LLC, Shreveport, Louisiana, 71105, United States|Minnesota Gastroenterology, PA, Maplewood, Minnesota, 55117, United States|Northwell Health Center for Liver Diseases and Transplantation, Manhasset, New York, 11030, United States|University of Rochester Medical Center, Rochester, New York, 14642, United States|The Liver Institute at Methodist Dallas Medical Center, Dallas, Texas, 75203, United States|University of Virginia Medical Center, Charlottesville, Virginia, 22908, United States|Bon Secours Richmond Community Hospital, Inc. d/b/a Bon Secours Liver Institute of Richmond, Richmond, Virginia, 23226, United States|VCU Clinical Research Services Unit (CRSU) [Patient Site Address], Richmond, Virginia, 23298, United States|University of Washington at Harborview Medical Center, Seattle, Washington, 98104, United States|Liver Institute Northwest, Seattle, Washington, 98105, United States Less <<
NCT02808312 Nonalcoholic Steatohepatitis (... More >>NASH)|Primary Sclerosing Cholangitis (PSC) Less << PHASE1 COMPLETED 2018-10-16 Miami, Florida, 33014, United ... More >>States|Orlando, Florida, 32809, United States|Knoxville, Tennessee, 37920, United States|San Antonio, Texas, 78215, United States|Auckland, 1640, New Zealand Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.52mL

1.70mL

0.85mL

17.04mL

3.41mL

1.70mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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