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 |
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| TP0472993
TP0472993 is a novel, orally active, selective inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis that inhibits the production of 20-HETE, thereby reducing the ERK1/2 and STAT3 signaling pathways, and ultimately inhibiting the progression of renal fibrosis. It can be used in studies related to chronic kidney disease (CKD). |
| Kushenol M
Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes. |
| Peucedanol
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively. |
| Methysticin
Methysticin is a major kavalactone in kava extract to induce CYP1A1. |
| Isoglycycoumarin
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochrome P450 2A6 (CYP2A6). |
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