MAP4K4-IN-3|1811510-58-3|-陌孚医药/Medlife

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MAP4K4-IN-3

目录号: PL06942 纯度: ≥99%

CAS No. :1811510-58-3

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中文名称	MAP4K4-IN-3
英文名称	MAP4K4-IN-3
英文别名	MAP4K4-IN-3;BDBM50134772;5-(6-Amino-5-(4-chlorophenyl)pyridin-3-yl)pyrimidin-2-amine
Cas No.	1811510-58-3
分子式	C₁₅H₁₂ClN₅
分子量	297.74
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	MAP4K4-IN-3 (Compound 17) 是一种有效的选择性 MAP4K4 抑制剂，在激酶实验中 IC₅₀ 为 14.9 nM，在细胞实验中 IC₅₀ 为 470 nM。具有抗糖尿病活性。
生物活性	MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC 50 of 14.9 nM in kinase assay, an IC 50 of 470 nM in cell assay. Antidiabetic agent.
性状	Solid
IC50 & Target[1][2]	MAP4K4 14.9 nM (IC50)
体外研究(In Vitro)	MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic agents. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Oral dosing in telemetered rats for 5 days with MAP4K4-IN-3 (Compound 2; 25 mg/kg, b.i.d.) results in a number of adverse effects. Substantial weight losses (7%) and body temperature increases (0.4°C) relative to controls are observed over the course of the study. For cardiovascular end points, maximal heart rate increases of 25 bpm, relative to controls, are induced by treatment with MAP4K4-IN-3. 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)
参考文献	[1]. Ammirati M, et al. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based AntidiabeticTreatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. [2]. Dow RL, et al. 2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety. J Med Chem. 2018 Apr 12;61(7):3114-3125.

溶解度数据	In Vitro: DMSO : 10 mg/mL (33.59 mM; ultrasonic and warming and heat to 60°C)配制储备液

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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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