MK-8245 - Stearoyl-CoA Desaturase (SCD) 抑制劑 - 生命科學(xué)試劑 - 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作靶點(diǎn): Stearoyl-CoA Desaturase (SCD)作通路: Metabolic Enzyme/Protease儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體

2、外實(shí)驗(yàn) DMSO : 19 mg/mL (40.66 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的?chǔ)備液，再依次添加

3、助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)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: 2.5 mg/mL (5.35 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.35 mM); Clear solution3. 請依序添加每種溶劑： 10% D

4、MSO 90% corn oilSolubility: 2.5 mg/mL (5.35 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 MK-8245種有效的，肝靶向的硬脂酰 -CoA 去飽和酶 (SCD) 抑制劑，對 SCD1 和 SCD1 的 IC50 值分別為 1 nM 和 3 nM，具有抗糖尿病和抗脂異常的功效 1。IC50 & Target IC50: 1 nM (human SCD1), 3 nM (rat SCD1), 3 nM (mouse SC

5、D1) 1體外研究 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.體內(nèi)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