MK-8245|1030612-90-8|-陌孚医药/Medlife

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MK-8245

目录号: PL11507 纯度: ≥98%

CAS No. :1030612-90-8

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中文名称	MK-8245
中文别名	2H-四唑乙酸,5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑];4-(2-溴-5-氟苯氧基)-1-[5-(2H-四唑-5-基)-3-唑基]哌啶;5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑基]-2H-四氮唑-2-乙酸;MK8245 抑制剂;5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑基]-2H-四氮唑-2-乙酸 98%
英文名称	MK-8245
英文别名	2-[5-[3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid;MK-8245;5-[3-[4-(2-bromo-5-fluorophenoxy)-1-piperidinyl]-5-isoxazolyl]-2H-Tetrazole-2-acetic acid;(5-{3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]isoxazol-5-yl}-2H-tetrazol-2-yl)acetic acid;(5-{3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]isoxazol-5-yl}tetrazol-2-yl)acetic acid;CS-0410;MK8245;UNII-537E7QE8LX;Aryl halide chemistry informer library compound X9;2-(5-(3-(4-(2-broMo-5-fluorophenoxy)piperidin-1-yl)isoxazol-5-yl)-2H-tetrazol-2-yl)acetic acid
Cas No.	1030612-90-8
分子式	C₁₇H₁₆N₆O₄FBr
分子量	467.25
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情

MK-8245 是一种有效的，肝靶向的硬脂酰 -CoA 去饱和酶 (SCD) 抑制剂，对人 SCD1 和鼠 SCD1 的 IC₅₀ 值分别为 1 nM 和 3 nM，具有抗糖尿病和抗血脂异常的功效。

生物活性

MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC 50 s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy.

性状

Solid

IC50 & Target[1][2]

IC50: 1 nM (human SCD1), 3 nM (rat SCD1), 3 nM (mouse SCD1)

体外研究(In Vitro)

MK-8245 is a potent and liver-specific SCD inhibitor.
MK-8245 displays similar potencies against human, rat and mouse SCD1, with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1.
MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, actives organic anion transporting polypeptides (OATPs) with IC50 of 68 nM, while being only weakly active OATPs in the HepG2 cell assay which is devoid of active with IC50 of ~1 μM.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

MK-8245 (10mg/kg; p.o.) exhibits a tissue distribution profile concentrated in the liver, with low exposure in tissues associated with potential adverse events in rats, dogs, and rhesus monkeys.
MK-8245 improves glucose clearance in a dose-dependent manner in eDIO mice administrated before the glucose challenge.
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, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

参考文献

[1]. Oballa RM, et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.J Med Chem. 2011 Jul 28;54(14):5082-96. Epub 2011 Jun 28.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (214.02 mM)配制储备液

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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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