MK-8245 - Stearoyl-CoA Desaturase (SCD) 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMK-8245Cat. No.: HY-13070CAS No.: 1030612-90-8分式: CHBrFNO分量: 467.25作靶点: Stearoyl-CoA Desaturase (SCD)作通路: Metabolic Enzyme/Protease储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体

2、外实验 DMSO : 19 mg/mL (40.66 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1402 mL 10.7009 mL 21.4018 mL5 mM 0.4280 mL 2.1402 mL 4.2804 mL10 mM 0.2140 mL 1.0701 mL 2.1402 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，配制前请先配制澄清的储备液，再依次添加

3、助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清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: 2.5 mg/mL (5.35 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.35 mM); Clear solution3. 请依序添加每种溶剂： 10% D

4、MSO 90% corn oilSolubility: 2.5 mg/mL (5.35 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 MK-8245种有效的，肝靶向的硬脂酰 -CoA 去饱和酶 (SCD) 抑制剂，对 SCD1 和 SCD1 的 IC50 值分别为 1 nM 和 3 nM，具有抗糖尿病和抗脂异常的功效 1。IC50 & Target IC50: 1 nM (human SCD1), 3 nM (rat SCD1), 3 nM (mouse SC

5、D1) 1体外研究 MK-8245 is a potent and liver-specific SCD inhibitor 1.MK-8245 displays similar potencies against human, rat and mouse SCD1, with IC50 values of 1 nM forhuman SCD1 and 3 nM for both rat SCD1 and mouse SCD1 1.MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which co

6、ntains functional, activesorganic anion transporting polypeptides (OATPs) with IC50 of 68 nM, while being only weakly active OATPsin the HepG2 cell assay which is devoid of active with IC50 of 1 M 1.体内研究 MK-8245 (10mg/kg; p.o.) exhibits a tissue distribution profile concentrated in the liver, with l

7、ow exposure intissues associated with potential adverse events in rats, dogs, and rhesus monkeys 1.MK-8245 improves glucose clearance in a dose-dependent manner in eDIO mice administrated before theglucose challenge 1.Animal Model: Male C57BL6 mice, male Sprague-Dawley rats 1Dosage: 10mg/kgAdministr

8、ation: Oral administrationResult: Exhibits a tissue distribution profile concentrated in the liver.REFERENCES1. Oballa RM, et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic windowfor the treatment of diabetes and dyslipidemia.J Med Chem. 2011 Jul 28;54(14):5082-96. Epub 2011 Jun 28.McePdfHeightCaution: Product has not been fully validated for medical applicati