Cilofexor is a potent, selective, orally active non-steroidal farnesoid X receptor (FXR) agonist with an EC50 value of 43 nM. It has anti-inflammatory activity and may be studied in primary sclerosing cholangitis (PSC) and non-alcoholic steatohepatitis (NASH).
| Molecular Weight | 552.4 |
| Formula | C28H23Cl2N3O5 |
| CAS Number | 1418274-28-8 |
| Solubility (25°C) | DMSO: ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Stergios A Polyzos, et al. Cilofexor for the Treatment of Nonalcoholic Steatohepatitis
| Related Farnesoid X Receptor Products |
|---|
| ASC-42
ASC-42 is a novel, potentially best-in-class, highly potent and selective non-steroidal FXR agonist that also inhibits the transcription of HBV RNA to hepatitis B surface antigen by inhibiting the transcription of HBV covalent closed-circle DNA (cccDNA) to HBV RNA. |
| Linafexor
Linafexor is a bile acid receptor (FXR) agonist that may be used in studies related to cholangitis and non-alcoholic steatohepatitis. |
| MET-409
MET-409 is an oral non-steroidal bile acid receptor FXR agonist for studies related to inflammatory bowel disease and irritable bowel syndrome. |
| FXR agonist 5
FXR agonist 5 is a FXR agonist. |
| XJ02862-S2
XJ02862-S2 shows potent FXR agonistic activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
