| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Cilofexor, formerly known as GS-9674, is a farnesoid X receptor (FXR) agonist. The nonsteroidal FXR agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with PSC. In clinical study, cilofexor was well tolerated and led to significant improvements in liver biochemistries and markers of cholestasis in patients with PSC.
| ln Vivo |
Cilofexor (GS-9674; 30 mg/kg; lateral wall gavage; once daily; for 10 weeks; stable Wistar stent) administration markedly enhanced Fgf15 expression in the ileum and decreased Cyp7a1 in the liver in non-alcoholic fatty liver disease (NASH). Significant reductions were observed in liver fibrosis and hepatic collagen expression. Without altering systemic hemodynamics, ciprofexor also considerably lowers portal pressure and hepatic stellate cell (HSC) activators [3].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats received a choline-deficient high-fat diet (CDHFD) [3]
Doses: 30 mg/kg Route of Administration: po (oral gavage); one time/day; for 10 weeks Experimental Results: Fgf15 expression in the ileum increased Dramatically, Cyp7a1 expression is diminished in the liver. Liver fibrosis and liver collagen expression were Dramatically diminished. |
| References |
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| Additional Infomation |
Cilofexor is under investigation in clinical trial NCT02943447 (Safety, Tolerability, and Efficacy of Cilofexor in Adults With Primary Biliary Cholangitis Without Cirrhosis).
Drug Indication Treatment of primary sclerosing cholangitis |
| Molecular Formula |
C28H22CL3N3O5
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|---|---|
| Molecular Weight |
586.85
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| Exact Mass |
585.062
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| CAS # |
1418274-28-8
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| Related CAS # |
2253764-93-9 (tromethamine);1418274-28-8 (free acid);
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| PubChem CID |
71228883
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
855.5±65.0 °C at 760 mmHg
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| Flash Point |
471.2±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.689
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| LogP |
4.98
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
39
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| Complexity |
867
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KZSKGLFYQAYZCO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H22Cl3N3O5/c29-20-2-1-3-21(30)24(20)25-18(26(39-33-25)15-4-5-15)12-38-17-6-7-19(22(31)11-17)28(37)13-34(14-28)23-10-16(27(35)36)8-9-32-23/h1-3,6-11,15,37H,4-5,12-14H2,(H,35,36)
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| Chemical Name |
2-(3-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)phenyl)-3-hydroxyazetidin-1-yl)isonicotinic acid
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| Synonyms |
Cilofexor GS-9674 GS 9674 GS9674
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~85.20 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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