Nevanimibe hydrochloride|133825-81-7|(PD-132301 hydrochloride; ATR101 hydrochloride)-陌孚医药/Medlife

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Nevanimibe hydrochloride (Synonyms: PD-132301 hydrochloride; ATR101 hydrochloride)

目录号: PL14731 纯度: ≥98%

CAS No. :133825-81-7

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中文名称	Nevanimibe hydrochloride
英文名称	Nevanimibe hydrochloride
英文别名	1-({1-[4-(dimethylamino)phenyl]cyclopentyl}methyl)-3-[2,6-di(propan-2-yl)phenyl]urea hydrochloride (1:1);1-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]-3-[2,6-di(propan-2-yl)phenyl]urea,hydrochloride;Nevanimibe hydrochloride;PD 132301-2;TK694ZFS57;1-(2,6-Diisopropylphenyl)-3-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride;Nevanimibe hydrochloride (USAN);Nevanimibe hydrochloride [USAN];PD132301-2;N-(2,6-Bis(1-methylethyl)phenyl)-N'-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea HCl
Cas No.	133825-81-7
分子式	C₂₇H₄₀ClN₃O
分子量	458.08
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Nevanimibe hydrochloride (PD-132301 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 (ACAT1) 抑制剂，EC₅₀ 为 9 nM。Nevanimibe hydrochloride 抑制 ACAT2，EC₅₀ 为 368 nM。Nevanimibe hydrochloride 诱导细胞凋亡 (apoptosis)，并具有抗肾上腺皮质癌的潜力。

生物活性

Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC 50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC 50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.

性状

Solid

IC50 & Target[1][2]

ACAT1 9 nM (EC50) ACAT2 368 nM (EC50

体外研究(In Vitro)

Coincubation of Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride; 3 nM-30 μM) and Cholesterol markedly increases toxicity in a dose-dependent manner, where 3 nM Nevanimibe in the presence of 60 μg/mL Cholesterol reduces survival by 60% after 24 hours. All doses of Nevanimibe (3 nM-30 μM) induces cytoxicity in the presence of Cholesterol, whereas treatment with Cholesterol in the absence of Nevanimibe has no effect on cell viability. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. LaPensee CR, et al. ATR-101, a Selective and Potent Inhibitor of Acyl-CoA Acyltransferase 1, Induces Apoptosis in H295R Adrenocortical Cells and in the Adrenal Cortex of Dogs. Endocrinology. 2016 May;157(5):1775-88.

溶解度数据	In Vitro: DMSO : 41.67 mg/mL (90.97 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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