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CYM 5541
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。
CYM 5541图片
CAS NO:945128-26-7
规格:98%
分子量:316.44
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
sphingosine-1-phosphate receptor 3 (S1P3) allosteric agonist
CAS:945128-26-7
分子式:C19H28N2O2
分子量:316.44
纯度:98%
存储:Store at -20°C

Background:

CYM-5541 (ML249) is an selective and allosteric S1P3 receptor agonist with an EC50 between 72 and 132 nM.


CYM-5541 is a full agonist, able to reach the maximum level of ERK phosphorylation that is observed with S1P. CYM-5541 has an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes: S1P1 EC50>10 μM, S1P2 EC50>50 μM, S1P4 EC50>50 μM, and S1P5 EC50>25 μM. CYM-5541 also shows selectivity over a large panel of protein targets, with no significant activities, in the Ricerca profiling panel of 55 GPCRs, ion channels, and transporters. CYM-5541 allowed us to identify an allosteric site where F263 is a key gate-keeper residue for its affinity and efficacy. The novel allosteric hydrophobic pocket may account for the S1P3 selectivity of CYM-5541[1].


参考文献:
[1]. Jo E, et al. Novel selective allosteric and bitopic ligands for the S1P(3) receptor. ACS Chem Biol. 2012 Dec 21;7(12):1975-83.