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AS 1949490
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。
AS 1949490图片
CAS NO:1203680-76-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
AS 1949490 是一种有效的、具有口服活性的选择性 SHIP2 磷酸酶抑制剂,对 Mouse SHIP2、Human SHIP2、Human SHIP1、Human PTEN、Human synaptojanin 和人肌管蛋白,分别。
Cas No.1203680-76-5
化学名(S)-3-((4-chlorobenzyl)oxy)-N-(1-phenylethyl)thiophene-2-carboxamide
Canonical SMILESClC1=CC=C(C=C1)COC2=C(C(N[C@@H](C)C3=CC=CC=C3)=O)SC=C2
分子式C20H18ClNO2S
分子量371.88
溶解度≥ 11.6mg/mL in DMSO
储存条件Store at RT
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

AS 1949490 is a selective inhibitor of Src homology 2 domain-containing inositol-5-phosphatase 2 (SHIP2), [1] with IC50 values of 0.34 μM and 0.62 μM to mouse and human SHIP2s, respectively [2].

SHIP2 is an intracellular phosphatase and appears to be important in insulin signaling as a negative regulator. SHIP2 has potential to act as a treatment for type 2 diabetes because of its inhibition [2].

Akt is a key enzyme to regulated insulin signaling. AS 1949490 treatment dose-dependently increased insulin-induced phosphorylation of Akt in L6 myotubes, but did not result in any associated changes in the overall level of Akt protein and the fetal bovine serum-induced phosphorylation of Akt. Treatments with AS 1949490 at several concentrations of and 1 nM insulin for 48 h, showed more consumption of glucose in the medium in a concentration-dependent manner [2].

In diabetic db/db mice, administered with AS 1949490 twice daily p.o. for 7 or 10 days significantly decreased plasma glucose (23% reduction, relative to vehicle), without affecting insulin levels, food intake or body weight. In the 10th day, treatment with AS 1949490 resulted in significant reduction in both the area under the blood glucose concentration time curve (AUC) and fasting blood glucose (37% reduction, compared with vehicle; time = -30 min) [2].

References:
[1].  Laura Beth J. McIntire, Kyu-In Lee, Belle Chang-IIeto, et al. Screening assay for small molecule inhibitors of synaptojanin 1, a synaptic phosphoinositide phosphatase. J Biomol Screen, 2014, 19(4):585-594.
[2].  A Suwa, T Yamamoto, A Sawada, et al. Discovery and functional characterization of a novel small molecule inhibitor of the intracellular phosphatase, SHIP2. British Journal of Pharmacology, 2009, 158:879-887.