HET0016 is a highly efficient and selective inhibitor of 20-HETE synthase, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1, CYP4A2 and CYP4A3, respectively. HET0016 is a selective CYP450 inhibitor that has been shown to inhibit angiogenesis and tumor growth.
| Molecular Weight | 206.28 |
| Formula | C12H18N2O |
| CAS Number | 339068-25-6 |
| Solubility (25°C) | DMSO : 5 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.
| 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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
