PF-06446846-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPF-06446846 hydrochlorideCat. No.: HY-120088ACAS No.: 1632250-50-0分式: CHClNO分量: 470.35作靶点: Ser/Thr Protease作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 250

2、mg/mL (531.52 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1261 mL 10.6304 mL 21.2608 mL5 mM 0.4252 mL 2.1261 mL 4.2522 mL10 mM 0.2126 mL 1.0630 mL 2.1261 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议

3、您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.42 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.42 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility

4、: 2.08 mg/mL (4.42 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 PF-06446846 hydrochloride种具有服活性，选择性前蛋转化酶枯草杆蛋酶/kexin 9 型 (PCSK9) 的翻译抑制剂。PF-06446846 hydrochloride 可通过诱导核糖体停在密码 34 周，从抑制PCSK9。IC50 & Target PCSK9 1体外研究 PF-06446846 inhibits the secretion of PC

5、SK9 by Huh7 cells with an IC50 of 0.3 M 1.体内研究 PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent mannerand lowers total cholesterol levels 1.Animal Model: Male Sprague-Dawley (Crl:CD SD rats, 6-8 wk old at initiation of dosing) 1Dosage: 5, 15, and 50 mg/kg

6、Administration: Oral gavage; daily for 14 daysResult: Lowered plasma PCSK9 in a dose-dependent manner and lowered total cholesterollevels.REFERENCES1. Lintner NG, et al. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain. PLoS Biol.2017 Mar 21;15(3):e2001882.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 4