CYM50260
Based on 1 Customer Validation
CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.94%
- CAS. Nr.: 1355026-60-6
- Formel: C14H11Cl3FNO2
- Molecular Weight:350.60
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Biologische Aktivität
EC50: 45 nM (S1P4-R)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | EC50 |
45 nM
Compound: 22aa, CYM50260
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Agonist activity at human S1P4R expressed in human U2OS cells containing EDG6 gene co-expressing GAL4-VP16 and beta-arrestin/TEV protease assessed as migration of VP16-GAL4 into nucleus by FERT based beta-lactamase reporter gene assay
Agonist activity at human S1P4R expressed in human U2OS cells containing EDG6 gene co-expressing GAL4-VP16 and beta-arrestin/TEV protease assessed as migration of VP16-GAL4 into nucleus by FERT based beta-lactamase reporter gene assay
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[PMID: 22119461] |
CYM50260 (Compound 22aa) is a synthetic S1P4-R agonist. CYM50260 is found 3.5-fold more potent than the hit compound (HTS-hit)[1].
CYM50260 suppresses the collagen-stimulated platelet aggregation, PDGF-AB secretion and sCD40L release. CYM50260 reduces the release of phosphorylated-HSP27 by collagen as well as the phosphorylation of HSP27[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1355026-60-6
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Appearance Solid
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Molecular Weight 350.60
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Formel C14H11Cl3FNO2
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Color White to off-white
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SMILES
FCC1=CC=C(OCCOC2=CC=C(Cl)C=C2Cl)C(Cl)=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (356.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Guerrero M, et al. Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P₄-R) agonists. Bioorg Med Chem Lett. 2012 Jan 1;22(1):537-42. [Content Brief]
[2]. Onuma T, et al. Sphingosine 1-phosphate (S1P) suppresses the collagen-induced activation of human platelets via S1P4 receptor. Thromb Res. 2017 Aug;156:91-100. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8523 mL | 14.2613 mL | 28.5225 mL | 71.3063 mL |
| 5 mM | 0.5705 mL | 2.8523 mL | 5.7045 mL | 14.2613 mL | |
| 10 mM | 0.2852 mL | 1.4261 mL | 2.8523 mL | 7.1306 mL | |
| 15 mM | 0.1902 mL | 0.9508 mL | 1.9015 mL | 4.7538 mL | |
| 20 mM | 0.1426 mL | 0.7131 mL | 1.4261 mL | 3.5653 mL | |
| 25 mM | 0.1141 mL | 0.5705 mL | 1.1409 mL | 2.8523 mL | |
| 30 mM | 0.0951 mL | 0.4754 mL | 0.9508 mL | 2.3769 mL | |
| 40 mM | 0.0713 mL | 0.3565 mL | 0.7131 mL | 1.7827 mL | |
| 50 mM | 0.0570 mL | 0.2852 mL | 0.5705 mL | 1.4261 mL | |
| 60 mM | 0.0475 mL | 0.2377 mL | 0.4754 mL | 1.1884 mL | |
| 80 mM | 0.0357 mL | 0.1783 mL | 0.3565 mL | 0.8913 mL | |
| 100 mM | 0.0285 mL | 0.1426 mL | 0.2852 mL | 0.7131 mL |
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