SR9186 (ML368) is a potent CYP3A4 inhibitor with IC50 s for inhibition of midazolam → 1′hydroxymidazolam, testosterone → 6β-hydroxytestosterone, and vincristine → vincristine M1 of 9, 4, and 38 nM, respectively. SR-9186 inhibits liver-stage development of P. falciparum to block ivermectin metabolism.
| Molecular Weight | 430.46 |
| Formula | C26H18N6O |
| CAS Number | 1361414-26-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 31.25 mg/mL (ultrasonic and warming and heat to 60°C) |
| 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.
| Related Cytochrome P450 (e.g. CYP17) Products |
|---|
| Cytochrome P450 reductase
Cytochrome P450 reductase is a NADPH-cytochrome reductase. |
| 20-SOLA
20-SOLA is a water-soluble 20-HETE antagonist. |
| TS-011
TS-011 is a selective inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis. |
| Dibromo-dodecenyl-methylsulfimide
Dibromo-dodecenyl-methylsulfimide is a selective inhibitor of 20-HETE synthesis and attenuates the vasodilatory response to sodium nitroprusside (SNP). |
| Abiraterone decanoate
Abiraterone decanoate is a novel, long-acting Abiraterone precursor compound that also exhibits high CYP17 cleavage enzyme inhibition selectivity for prostate cancer related studies. |
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