Biochem/physiol Actions
HET0016 is a potent and selective inhibitor against cytochrome P450 (CYP450) ω-hydroxylases (human CYP4A11/4A22/4F2/4F3, rat CYP4A1/4A2/4A3/4A8)-mediated 20-hydroxyeicosatetraenoic acid (20-HETE) biosynthesis (IC50 = 8.9/35 nM using human/rat renal microsomes), exhibiting much reduced potency against epoxyeicosatrienoic acids (EETs) biosynthesis (IC50 = 2.8 μM/rat microsome) or the enzyme activities of CYP2C9/2D6/3A4 and COX (IC50 = 3.3/83.9/71 μM and 2.3 μM). HET0016 is widely employed both in cultures (1-10 μM) and in aminals in vivo (1-10 mg/kg via i.v., i.m., i.p. or s.c.) for probing 20-HETE-dependent physiological and pathological processes.
Potent and selective inhibitor against cytochrome P450 (CYP450) ω-hydroxylases-mediated 20-hydroxyeicosatetraenoic acid (20-HETE) biosynthesis.
| assay | ≥95% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | CCCCC1=CC=C(C(C)=C1)/N=C/NO |
| InChI | 1S/C12H18N2O/c1-3-4-5-11-6-7-12(10(2)8-11)13-9-14-15/h6-9,15H,3-5H2,1-2H3,(H,13,14) |
| InChI key | LYNOGBKNFIHKLE-UHFFFAOYSA-N |
