|N,N-二环己基-5-环丙基异恶唑-3-甲酰胺|CsnPharm

CAS No.: 945128-26-7

CYM-5541 Catalog No. CSN20443

Synonyms: ML249;CID 17253208

CYM-5541 is an allosteric agonist of S1P3 with EC50 of 72 nM - 132 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 S1PR3

EC50:72nM~132nM
描述Sphingosine 1-phosphate 3 (S1P₃) receptor is distributed on cardiac myocytes and cardiac fibroblasts in vivo and it plays a critical role in cardiovascular physiology, especially pace-making activity. CYM 5541 is a full S1P₃-selective agonist, able to reach the maximum level of ERK phosphorylation that was observed with S1P. CYM-5541 has an EC₅₀ of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P₁ EC₅₀ > 10 μM, S1P₂ EC₅₀ > 50 μM, S1P₄ EC₅₀ > 50 μM, and S1P₅ EC₅₀ > 25 μM^[3]. 10 nM of CYM5541 promotes the proliferation and attenuates apoptosis of bone marrow (BM)-derived Endothelial progenitor cells induced by H2O2Wang H, Huang H, Ding SF. Sphingosine-1-phosphate promotes the proliferation and attenuates apoptosis of Endothelial progenitor cells via S1PR1/S1PR3/PI3K/Akt pathway. Cell Biol Int. 2018 Nov;42(11):1492-1502. doi: 10.1002/cbin.10991.
作用机制CYM 5541 sits in the hydrophobic pocket close to F263^[3].
参考文献

[1] Jo E, Bhhatarai B, et al. Novel selective allosteric and bitopic ligands for the S1P(3) receptor. ACS Chem Biol. 2012 Dec 21;7(12):1975-83.
[2] Guerrero M, Poddutoori R, et al. Probe Development Efforts for an Allosteric Agonist of the Sphingosine 1-phosphate Receptor 3 (S1P3). 2011 Aug 31 [updated 2013 Feb 25] . Probe Reports from the NIH Molecular Libraries Program [Internet] .
[3] Jo E, Bhhatarai B, Repetto E, et al. Novel selective allosteric and bitopic ligands for the S1P(3) receptor. ACS Chem Biol. 2012 Dec 21;7(12):1975-83

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1602 mL
- 15.8009 mL
- 31.6018 mL
- 5 mM
- 0.6320 mL
- 3.1602 mL
- 6.3204 mL
- 10 mM
- 0.3160 mL
- 1.5801 mL
- 3.1602 mL

技术信息

CAS号

945128-26-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H28N2O2

运输

蓝冰

分子量

316.44

别名

ML249;CID 17253208

溶解度

DMSO	32.0 mg/mL (101.1 mM)
Water	Insoluble
Ethanol	63.0 mg/mL (199.1 mM)

动物实验配方

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