الصفحة الرئيسية>>Signaling Pathways>> GPCR/G protein>> S1P receptor inhibitor>>ML-178

ML-178 (Synonyms: CID 44620892,CYM 50179,SID 87544119)

رقم الكتالوجGC10433 Copy One-Click Copy Product Info

ML-178 (المركب 22n) هو ناهض قوي وانتقائي S1P4-R (مستقبلات Sphingosine-1-phosphate4) مع EC50 من 46 نانومتر.

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ML-178 التركيب الكيميائي

Cas No.: 1355026-47-9

الحجم السعر المخزون الكميّة
1mg
49٫00
متوفر
5mg
132٫00
متوفر
10mg
236٫00
متوفر
25mg
528٫00
متوفر

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مراجعات العميل

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Sample solution is provided at 25 µL, 10mM.



Description of ML-178

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].

Chemical Properties of ML-178

Cas No. 1355026-47-9 SDF
المرادفات CID 44620892,CYM 50179,SID 87544119
Chemical Name 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
Formula C13H9Br2Cl2NO2 M.Wt 441.9
الذوبان ≤15mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ML-178

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.263 mL 11.3148 mL 22.6296 mL
5 mM 452.6 μL 2.263 mL 4.5259 mL
10 mM 226.3 μL 1.1315 mL 2.263 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Review for ML-178

Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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