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MAP4K4-IN-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MAP4K4-IN-3图片
CAS NO:1811510-58-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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。
Cas No.1811510-58-3
分子式C15H12ClN5
分子量297.74
溶解度DMSO : 10 mg/mL (33.59 mM; ultrasonic and warming and heat to 60°C)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay. Antidiabetic agent[1].

MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic agents[1].

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[2].

[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.