Cilofexor
- Product Name
- 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;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
- Formula Weight
- 586.85
- MOL File
- 1418274-28-8.mol
Cilofexor Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 25747
- Product name
- Cilofexor
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $39
- Updated
- 2024/03/01
- Product number
- 25747
- Product name
- Cilofexor
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $202
- Updated
- 2024/03/01
- Product number
- 25747
- Product name
- Cilofexor
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $363
- Updated
- 2024/03/01
- Product number
- 25747
- Product name
- Cilofexor
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $745
- Updated
- 2024/03/01
- Product number
- CS-0039260
- Product name
- Cilofexor
- Purity
- 99.82%
- Packaging
- 50mg
- Price
- $840
- Updated
- 2021/12/16
Cilofexor Chemical Properties,Usage,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
Cilofexor Suppliers
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View Lastest Price from Cilofexor manufacturers
- Product
- Cilofexor 1418274-28-8
- Price
- US $9.80/KG
- Min. Order
- 1KG
- Purity
- 97%-99%
- Supply Ability
- 1kg -1000kg
- Release date
- 2020-01-02