ML-178 (Synonyms: CID 44620892,CYM 50179,SID 87544119) |
カタログ番号GC10433
One-Click Copy Product Info
|
ML-178 (化合物 22n) は、46 nM の EC50 を持つ強力かつ選択的な S1P4-R (スフィンゴシン-1-リン酸 4 受容体) アゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1355026-47-9
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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 | |
| 同義語 | 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 |
| 溶解度 | ≤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. | ||
| 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)