Nevanimibe hydrochloride (PD-132301 hydrochloride) 是选择性酰基辅酶 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。 体外活性： 在H295R人源肾上腺皮质癌细胞中，Nevanimibe hydrochloride(ATR-101 hydrochloride)能够降低胆固醇酯的形成并提升游离胆固醇(FC)水平，显示出对ACAT1活性的强效抑制。ATR-101处理还导致Caspase-3/7水平上升和末端脱氧核糖核酸转移酶2'-脱氧尿苷5'-三磷酸镍末端标记阳性细胞增加，这表明激活了细胞凋亡。 Nevanimibe hydrochloride ( PD-132301 hydrochloride ) is a selective acyl-CoA : cholesterol O-acyltransferase 1 inhibitor with an EC50 of 9 nM. It inhibits ACAT2 with an EC50 of 368 nM. It induces apoptosis and has the potential to resist adrenocortical carcinoma. In vitro activity 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.
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Nevanimibe hydrochloride（PD-132301 hydrochloride）
CAS number：133825-81-7 molecular formula：C27H40ClN3O
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| Chinese alias | 盐酸奈伐尼米布 | ||
| English alias | PD132301-02 | ATR101 hydrochloride | PD 132301-02 | 1[[1[4(Dimethylamino)phenyl]cyclopentyl]methyl]3[2,6di(propan2yl)phenyl]urea hydrochloride | PD 132301-2 | PD132301-2 | PD132301 HCl | CI-984 | N-[2,6-bis(1-Methylethyl)phenyl]-N-[[1-[4-(dimethylamino)ph | ||
| CAS number | 133825-81-7 | molecular formula | C27H40ClN3O |
| molecular weight | 458.08 g/mol | Exact mass | - |
| PSA | 44.400 Ų | logp | - |
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