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CYM 5541 Sale

(Synonyms: ML249) 目录号 : GC16946

A selective agonist of S1P3

CYM 5541 Chemical Structure

Cas No.:945128-26-7

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

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].

References:

[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.

产品描述

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].

References:
[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.

Chemical Properties

Cas No. 945128-26-7 SDF
别名 ML249
化学名 N,N-dicyclohexyl-5-cyclopropylisoxazole-3-carboxamide
Canonical SMILES O=C(N(C1CCCCC1)C2CCCCC2)C3=NOC(C4CC4)=C3
分子式 C19H28N2O2 分子量 316.44
溶解度 DMSO: 5 mg/ml 储存条件 Store at -20°C
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1 mM 3.1602 mL 15.8008 mL 31.6016 mL
5 mM 0.632 mL 3.1602 mL 6.3203 mL
10 mM 0.316 mL 1.5801 mL 3.1602 mL
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