Nevanimibe-hydrochloride-PD-132301-hydrochloride-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENevanimibe hydrochlorideCat. No.: HY-100399ACAS No.: 133825-81-7Synonyms: PD-132301 hydrochloride; ATR101 hydrochloride分式: CHClNO分量: 458.08作靶點: Acyltransferase作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn so

2、lvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 41.67 mg/mL (90.97 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1830 mL 10.9151 mL 21.8302 mL5 mM 0.4366 mL 2.1830 mL 4.3660 mL10 mM 0.2183 mL 1.0915 mL 2.1830 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選

3、擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.54 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.54 mM); Clea

4、r solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (4.54 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride)種有效的選擇性?；o酶 A：膽固醇 O-酰基轉(zhuǎn)移酶 1 (ACAT1) 抑制劑，EC50 為 9 nM。Nevanimibe

5、hydrochloride (PD-132301hydrochloride; ATR101 hydrochloride) 抑制 ACAT2，EC50 為 368 nM 1。IC50 & Target ACAT1 ACAT29 nM (EC50) 368 nM (EC50)體外研究 Coincubation of Nevanimibe (ATR-101; 3 nM-30 M) and Cholesterol markedly increases toxicity in a dose-dependent manner, where 3 nM Nevanimibe in the presence o

6、f 60 g/mL Cholesterol reduces survival by60% after 24 hours. All doses of Nevanimibe (3 nM-30 M) induces cytoxicity in the presence of Cholesterol,whereas treatment with Cholesterol in the absence of Nevanimibe has no effect on cell viability 1.Cell Cytotoxicity Assay 1Cell Line: The H295R and HAC c

7、lone 15 (HAC15) human ACC cell linesConcentration: 3 nM-30 MIncubation Time: 24 hoursResult: 3 nM-3 M exhibited no toxicity, whereas 30 M treatment reduced survival byapproximately 40% within 24 hours.REFERENCES1. LaPensee CR, et al. ATR-101, a Selective and Potent Inhibitor of Acyl-CoA Acyltransferase 1, Induces Apoptosis in H295RAdrenocortical Cells and in the Adrenal Cortex of Dogs. Endocrinology. 2016 May;157(5):1775-88.McePdfHeightCaution: Product has not been fully validated for medical applications.For res