CYM 5541

产品编号 T3961   CAS 945128-26-7
别名: ML249, CID-17253208

CYM-5541 is a selective and allosteric S1P3 receptor agonist.

CYM 5541结构式
CYM 5541 , CAS 945128-26-7
规格 库存 价格/RMB 数量
2 mg 上海现货 361.00
5 mg 上海现货 651.00
10 mg 上海现货 1107.00
25 mg 上海现货 2437.00
50 mg 上海现货 4337.00
100 mg 上海现货 7377.00
1 mL * 10 mM (in DMSO) 上海现货 651.00
存储 & 溶解度
产品描述 CYM-5541 is a selective and allosteric S1P3 receptor agonist.
靶点活性 S1P3 : EC50:between72and132nM,  
体外活性 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].
Kinase Assay Jump-In TI CHO-K cells stably expressing WT or mutant S1P3 are serum-starved for 4 hrs. They are then incubated at 4 °C for 30 min in the binding buffer containing 20 mM Tris-HCl (pH 7.5), 100 mM NaCl, 15 mM NaF, 0.5 mM EDTA, 1 mM Na3VO4, 0.5% fatty acid-free bovine serum albumin, and protease inhibitor mixture with 0.1 nM [33P]S1P and increasing concentrations of S1P, SPM-242, or CYM-5541. Cells are washed three times with cold binding buffer. Cell-bound radioactivity is measured by lysing the cells with 0.5% SDS followed by liquid scintillation counting. The raw data is normalized so that the level of [33P]S1P bound to each cell line (WT or mutant) in the absence of competing ligand is referenced as 100% for its own cell line[1].
别名 ML249, CID-17253208
纯度 97.34%
分子量 316.44
分子式 C19H28N2O2
CAS No. 945128-26-7


0-4℃ for short term (days to weeks), or -20℃ for long term (months).


DMSO: 39 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )


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.

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This product is contained In the following compound libraries:
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