N’-(4-Butyl-2-methylphenyl)-N-hydroxyformimidamide , ≥95% , 339068-25-6

CAS NO.：339068-25-6

Empirical Formula: C12H18N2O

Molecular Weight: 206.28

MDL number: MFCD00277704

PRODUCT Properties

• Melting point: 138-140°C
• storage temp.: Hygroscopic, -20°C Freezer, Under inert atmosphere
• solubility: Chloroform (Slightly), Ethanol (Slightly)
• form: Light pink solid.
• color: White to Pale Yellow
• CAS DataBase Reference: 339068-25-6

Description and Uses

20-HETE is a major biologically active cytochrome P450 (CYP450) metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an IC₅₀ of 8.9 nM, selectively inhibiting CYP4A and 4F isoforms. HET0016 inhibits CYP2C9, CYP2D6, and CYP3A4, enzymes important in drug metabolism, significantly less effectively with IC₅₀s in the μM range. The IC₅₀ values for inhibition of cyclooxygenase and epoxyeicosatrienoic acids (EETs) formation are 2.3 and 2.8 μM, respectively.

HET-0016 is a potent and selective inhibitor of the biosynthesis of 20-HETE acting via inhibition of CYP4A (IC50=8.9nM (human), 35nM (rat renal microsome). IC50 cyclooxygenase=2.3uM. IC50 for other CYP’s: CYP2C9-3.3uM, CYP2D6=83.9 uM, CYP3A4=71uM. It inhibits cerebrovascular constriction induced by Ca2+ or archidonate and inhibits angiogenesis and endothelial cell sprouting in various models. Displays protective effect on brain damage after temporary focal ischemia (at 10mg/Kg).

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H315-H319-H335
• Precautionary statements: P261-P280a-P304+P340-P305+P351+P338-P405-P501a