CYM 5520_S1P2的非竞争性变构激动剂_1449747-00-5_Apexbio

产品名: CYM 5520修订日期: 6/30/2016产品说明书

化学性质

产品名:

CYM 5520 //struct// Cas No.:

1449747-00-5 分子量:

345.4 分子式:

C21H19N3O2 化学名:

1-[2-[2,5-dimethyl-1-(phenylmethyl)-1H-pyrrol-3-yl]-2-oxoethyl]-1,6-dihydro-6-oxo-3-pyridinecarbonitrile SMILES:

O=C1C=CC(C#N)=CN1CC(C2=C(C)N(CC3=CC=CC=C3)C(C)=C2)=O 溶解性:

Soluble in DMSO 储存条件:

Store at -20°C 一般建议: For obtaining a higher solubility , please warm the tube at 37°C

and shake it in the ultrasonic bath for a while.Stock solution can be

stored below -20°C for several months.

运输条件:

Evaluation sample solution : ship with blue ice

All other available size: ship with RT , or blue ice upon request

生物活性

靶点 :

GPCR/G protein 信号通路:

S1P receptor inhibitor 产品描述:

CYM 5520 is a potent, specific and noncompetitive allosteric agonist of sphingosine 1-phosphate receptor 2 (S1P2) without showing any agonist activity towards S1P1, S1P3, S1P4 or S1P5.

Sphingosine 1-phosphate (S1P) is an extracellular lipid mediator and the major effects of S1P are mediated via five distinct G protein-coupled receptors, including S1P1/EDG-1, S1P2/EDG-5,

S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. S1P2 is involved in a variety of biological processes, including cell proliferation, migration, survival, and differentiation.

In vitro: CYM 5520 showed selective agonist activity towards wild type S1P2 and triple mutant

S1P2 expressed in cells with an EC50 of 1.6 μM and 1.5μM, respectively. Also, CYM 5520 were inactive towards S1P1, S1P3, S1P4 or S1P5. In addition, CYM 5520 did not inhibit S1P binding and was not competitive with SIP [1]. In human pancreatic cancer cell line, CFPAC-1 cells, the frequency of basal extrusion in p120 catenin-deficient spheres was reduced significantly by the treatment of CYM 5520 to levels similar to those observed in p120 catenin-expressing spheres [2].

In vivo: Up to now, in vivo study of CYM 5520 is still in the development stage.

参考文献:

特别声明

产品仅用于研究，

不针对患者销售，望谅解。

每个产品具体的储存和使用信息显示在产品说明书中。ApexBio产品在推荐的条件下是稳定的。产品会根据不同的推荐温度进行运输。许多产品短期运输是稳定的，运输温度不同于长期储存的温度。我们确保我们的产品是在保持试剂质量的条件下运输的。收到产品后，按照产品说明书上的要求进行储存。

ApexBio Technology