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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Cytochrome P450 (CYPs)-HET0016
HET0016

Chemical Structure : HET0016

CAS No.: 339068-25-6

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HET0016 (HET 0016, HET-0016)

货号: PC-35319Not For Human Use, Lab Use Only.

HET0016 (HET-0016) is a potent, selective inhibitor of CYP4A, potently inhibits the formation of 20-HETE with IC50 of 8.9 nM in human renal microsomes.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HET0016 (HET-0016) is a potent, selective inhibitor of CYP4A, potently inhibits the formation of 20-HETE with IC50 of 8.9 nM in human renal microsomes.
HET0016 inhibits 20-HETE formation in rat renal microsomes with IC50 of 35 nM, shows no significant inhibition of the formation of epoxyeicosatrienoic acids (IC50=2,800 nM).
HET0016 also inhibits the CYP2C9, CYP2D6 and CYP3A4-catalysed substrates oxidation at higher concentrations (IC50=3,300, 83,900 and 71,000 nM).
HET0016 reduces protein tyrosine and p42/p44 MAPK phosphorylation, significantly inhibits the U251 proliferation and phosphorylation of both the EGFR and p42/p44 MAPK induced by EGF.
HET0016 suppresses 9L gliosarcoma cell proliferation and tumor growth in rats.

物理化学性质&存储条件

分子量 206.289
分子式 C12H18N2O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(4-butyl-2-methylphenyl)-N'-hydroxy-methanimidamide

参考文献

1. Sato M, et al. Bioorg Med Chem Lett. 2001 Dec 3;11(23):2993-5.

2. Guo M, et al. J Pharmacol Exp Ther. 2005 Nov;315(2):526-33.

3. Miyata N, et al. Br J Pharmacol. 2001 Jun;133(3):325-9.

4. Guo M, et al. J Pharmacol Exp Ther. 2006 Apr;317(1):97-108.

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