Cilofexor
- CAS No.
- 1418274-28-8
- Chemical Name:
- Cilofexor
- Synonyms
- CS-2761;Cilofexor;Cilofexor （GS-9674);Cilofexor, 10 mM in DMSO;GS-9674;GS9674;CILOFEXOR;2-(3-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)phenyl)-3-hydroxyazetidin-1-yl)isonicotinic acid;2-[3-[2-Chloro-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]phenyl]-3-hydroxy-1-azetidinyl]-4-pyridinecarboxylic acid;GS9674,Inhibitor,inhibit,NR1H4,FXR,Cilofexor,PSC,GS 9674,oral,NASH,GS-9674,antifibrotic,nonsteroidal,anti-inflammatory,Autophagy,safety;4-Pyridinecarboxylic acid, 2-[3-[2-chloro-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]phenyl]-3-hydroxy-1-azetidinyl]-;2-[3-(2-chloro-4-{[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy}phenyl)-3-hydroxyazetidin-1-yl]pyridine-4-carboxylic acid
- CBNumber:
- CB23956597
- Molecular Formula:
- C28H22Cl3N3O5
- Molecular Weight:
- 586.85
- MDL Number:
- MFCD31731099
- MOL File:
- 1418274-28-8.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Boiling point | 855.5±65.0 °C(Predicted) |
|---|---|
| Density | 1.538±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO:32.5(Max Conc. mg/mL);55.38(Max Conc. mM) |
| form | A crystalline solid |
| pka | 2.10±0.10(Predicted) |
| color | Off-white to light yellow |
| InChIKey | KZSKGLFYQAYZCO-UHFFFAOYSA-N |
| SMILES | C1(N2CC(C3=CC=C(OCC4=C(C5CC5)ON=C4C4=C(Cl)C=CC=C4Cl)C=C3Cl)(O)C2)=NC=CC(C(O)=O)=C1 |
| FDA UNII | YUN2306954 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
Cilofexor price More Price(48)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 25747 | Cilofexor ≥98% | 1418274-28-8 | 1mg | $43 | 2026-04-30 | Buy |
| Cayman Chemical | 25747 | Cilofexor ≥98% | 1418274-28-8 | 5mg | $223 | 2026-04-30 | Buy |
| Cayman Chemical | 25747 | Cilofexor ≥98% | 1418274-28-8 | 10mg | $400 | 2026-04-30 | Buy |
| Cayman Chemical | 25747 | Cilofexor ≥98% | 1418274-28-8 | 25mg | $820 | 2026-04-30 | Buy |
| Biosynth | TGC27428 | Cilofexor | 1418274-28-8 | 25mg | $1370.5 | 2026-06-05 | Buy |
Cilofexor Chemical Properties, Uses, Production
Description
Cilofexor inhibits binding of a synthetic peptide, comprising residues 676-700 of the steroid receptor coactivator 1 (SRC-1), to the farnesoid X receptor (FXR; EC50 = <25 nM in a FRET activity assay). It has FXR agonist activity in a mammalian one hybrid (M1H) assay (EC50 = ≥100 nM).
Uses
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].
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].
| 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. |
References
[1] Trauner M, et al. The Nonsteroidal Farnesoid X Receptor Agonist Cilofexor (GS-9674) Improves Markers of Cholestasis and Liver Injury in Patients With Primary Sclerosing Cholangitis. Hepatology. 2019 Sep;70(3):788-801. DOI:10.1002/hep.30509
[2] Patel K, et al. Cilofexor, a Nonsteroidal FXR Agonist, in Non-Cirrhotic Patients with Nonalcoholic Steatohepatitis: A Phase 2 Randomized Controlled Trial. Hepatology. 2020 Mar 1. DOI:10.1002/hep.31205
[3] P. Schwab, et al. The FXR agonist GS-9674 reduces fibrosis and portal hypertension in a rat model of NASH. April 2018,Volume 68, Supplement 1, Pages S471-S472.
Cilofexor Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Chengdu DingDang Pharmaceutical Co., Ltd. | 028-86040038 | market@dingdangchem.com | China | 1853 | 55 |
| Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd | 15317229551 | 15151849396@163.com | China | 975 | 58 |
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 | sales@sun-shinechem.com | China | 1197 | 64 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3493 | 58 |
| Bide Pharmatech Ltd. | 400-164-7117 18317119277 | product02@bidepharm.com | China | 40000 | 60 |
| Hangzhou J&H Chemical Co., Ltd. | 0571-87396432 | sales@jhechem.com | China | 14905 | 59 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4859 | 55 | |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| ShangHai Biochempartner Co.,Ltd | 177-54423994 17754423994 | 2853530910@QQ.com | China | 8000 | 62 |
| Shanghai SuperLan Chemcial Technique Centre | 0-2022843681 15618226720 | chaolaichem@foxmail.com | China | 9996 | 58 |
