ML-178
(Synonyms: CID 44620892,CYM 50179,SID 87544119) 目录号 : GC10433A selective S1P4 agonist
Cas No.:1355026-47-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ML-178 is a novel and selective S1P4 activator with EC50 value of 46.3 nM [1].
Sphingosine-1-phosphate (S1P) is an extracellular lipid mediator released by activated blood platelets that serves to influence heart rate, coronary artery caliber, endothelial integrity, lung epithelial integrity and lymphocyte recirculation through five of the S1P receptors (S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8). S1P4 receptor is coupled to Gαi and Gαo G proteins and activates ERK, MAPK and PLC downstream pathways [1].
ML-178 is a novel and selective S1P4 activator. ML178 activated S1P4 receptor with an EC50 of 46.3 nM, and is inactive against other members of the receptor family, with EC50s > 50 μM against S1P1, S1P2, S1P3, and S1P5 receptors. ML178 was inhibited by an S1P4 receptor-selective antagonist with an IC50 of 0.83 μM. ML178 was nontoxic to U2OS cells with a CC50 of > 20 μM. ML178 was generally inactive against a broad array of off targets, including receptors, transporters, or ion channels [1].
Reference:
[1]. Guerrero M, Urbano M, Velaparthi S, et al. Probe Development Efforts to Identify Novel Agonists of the Sphingosine 1-phosphate Receptor 4 (S1P4). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.2010 Oct 12 [updated 2011 Dec 12].
Cas No. | 1355026-47-9 | SDF | |
别名 | CID 44620892,CYM 50179,SID 87544119 | ||
化学名 | 2,6-dibromo-3-[2-(2,4-dichlorophenoxy)ethoxy]-pyridine | ||
Canonical SMILES | ClC1=CC(Cl)=C(OCCOC2=C(Br)N=C(Br)C=C2)C=C1 | ||
分子式 | C13H9Br2Cl2NO2 | 分子量 | 441.9 |
溶解度 | ≤15mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.263 mL | 11.3148 mL | 22.6296 mL |
5 mM | 0.4526 mL | 2.263 mL | 4.5259 mL |
10 mM | 0.2263 mL | 1.1315 mL | 2.263 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。