Molecular structure of HET-0016, CAS Number: 339068-25-6
HET-0016 (CAS 339068-25-6)
See product citations (5)
Alternate Names:
N-Hydroxy-N-(4-butyl-2-methylphenyl)formamidine
Application:
HET-0016 is a potent and selective inhibitor of the biosynthesis of 20-HETE
CAS Number:
339068-25-6
Purity:
≥98%
Molecular Weight:
206.28
Molecular Formula:
C12H18N2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
A potent and selective inhibitor of the biosynthesis of 20-HETE in human renal microsomes with an IC50 of 8.9 nM, selectively inhibiting CYP4A and 4F isoforms. HET0016 inhibits CYP2C9, CYP2D6, and CYP3A4: enzymes that are 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. It also inhibits cerebrovascular constriction induced by calcium or arachidonate and inhibits angiogenesis and endothelial cell sprouting in various models.
HET-0016 (CAS 339068-25-6) References
- HET0016, a potent and selective inhibitor of 20-HETE synthesizing enzyme. | Miyata, N., et al. 2001. Br J Pharmacol. 133: 325-9. PMID: 11375247
- 20-HETE contributes to the acute fall in cerebral blood flow after subarachnoid hemorrhage in the rat. | Kehl, F., et al. 2002. Am J Physiol Heart Circ Physiol. 282: H1556-65. PMID: 11893593
- CYP4A metabolites of arachidonic acid and VEGF are mediators of skeletal muscle angiogenesis. | Amaral, SL., et al. 2003. Am J Physiol Heart Circ Physiol. 284: H1528-35. PMID: 12521947
- Smooth muscle--specific expression of CYP4A1 induces endothelial sprouting in renal arterial microvessels. | Jiang, M., et al. 2004. Circ Res. 94: 167-74. PMID: 14670847
- Calcium transients in astrocyte endfeet cause cerebrovascular constrictions. | Mulligan, SJ. and MacVicar, BA. 2004. Nature. 431: 195-9. PMID: 15356633
- Cytochrome P-450 metabolites in renal circulation and excretion--interaction with the nitric oxide (NO) system. | Kompanowska-Jezierska, E. and Kuczeriszka, M. 2008. J Physiol Pharmacol. 59 Suppl 9: 137-49. PMID: 19261977
- Role of cytochrome P-450 metabolites in the regulation of renal function and blood pressure in 2-kidney 1-clip hypertensive rats. | Sporková, A., et al. 2011. Am J Physiol Regul Integr Comp Physiol. 300: R1468-75. PMID: 21411763
- Effect of 20-HETE inhibition on L-NAME-induced hypertension in rats. | Özen, N., et al. 2018. Clin Exp Hypertens. 40: 292-302. PMID: 29087727
- The contribution of TRPV1 channel to 20-HETE-Aggravated ischemic neuronal injury. | Zhang, X., et al. 2018. Prostaglandins Other Lipid Mediat. 137: 63-68. PMID: 30041768
- The role of SHP/REV-ERBα/CYP4A axis in the pathogenesis of alcohol-associated liver disease. | Yang, Z., et al. 2021. JCI Insight. 6: PMID: 34423788
- A convenient test system for the identification of CYP4V2 inhibitors. | Sharma, S., et al. 2021. Mol Vis. 27: 601-607. PMID: 34880593
- Activation of 20-HETE Synthase Triggers Oxidative Injury and Peripheral Nerve Damage in Type 2 Diabetic Mice. | Haddad, M., et al. 2022. J Pain. 23: 1371-1388. PMID: 35339661
- The interaction between STING and NCOA4 exacerbates lethal sepsis by orchestrating ferroptosis and inflammatory responses in macrophages. | Wu, J., et al. 2022. Cell Death Dis. 13: 653. PMID: 35902564
Inhibitor of:
Angiogenesis, Cox, CYP, and CYP4A11.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
HET-0016, 1 mg | sc-200673B | 1 mg | $24.00 | |||
HET-0016, 5 mg | sc-200673 | 5 mg | $99.00 | |||
HET-0016, 10 mg | sc-200673D | 10 mg | $147.00 | |||
HET-0016, 25 mg | sc-200673A | 25 mg | $388.00 | |||
HET-0016, 100 mg | sc-200673C | 100 mg | $1102.00 |