Nevanimibe hydrochloride 是一种口服有效的,选择性酰基辅酶 A:胆固醇 O-酰基转移酶 1 抑制剂,EC50为 9 nM。它抑制 ACAT2,EC50为 368 nM。它诱导细胞凋亡,具有抗肾上腺皮质癌的潜力。
产品描述
Nevanimibe hydrochloride is an orally active and selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) (EC50 of 9 nM).
体外活性
In H295R human adrenocortical carcinoma cells, Nevanimibe hydrochloride(ATR-101 hydrochloride) decreases the formation of cholesteryl esters and increases FC levels, demonstrating potent inhibition of ACAT1 activity.?Caspase-3/7 levels and terminal deoxynucleotidyl transferase 2'-deoxyuridine 5'-triphosphate nick end labeled-positive cells are increased by ATR-101 treatment, indicating activation of apoptosis[2].
Cas No.
133825-81-7
分子式
C27H40ClN3O
分子量
458.08
别名
PD-132301 hydrochloride;ATR101 hydrochloride
储存和溶解度
DMSO:41.67 mg/mL (90.97 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years