CYM5442
Based on 5 publication(s) in Google Scholar
CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS).
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- 純度: 98.83%
- CAS 番号: 1094042-01-9
- 分子式: C23H27N3O4
- 分子量:409.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
EC50: 1.35 nM (Sphingosine 1-phosphate (S1P1) receptor)[1]
CYM5442 (0.5 μM; 0-60 minutes; HEK293 cells) treatment stimulates S1P1 phosphorylation in a time-dependent manner in P32-orthophosphate labeled cells[1].
CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation in CHO-K1 cells transfected with S1P1 with an EC50 of 46 nM. The R120 for alanine (R120A) mutant is still able to maintain p42/p44-MAPK activity when incubated with CYM5442 (EC50 of 67 nM). Activation of p42/p44-MAPK by CYM5442 in E121A S1P1 cells is concentration dependent, with a mean EC50 value of 134 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells stably expressing S1P1 fused to GFP on the carboxy-terminus
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Concentration:0.5 µM
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Incubation Time:0 minutes, 2 minutes, 5 minutes, 10 minutes, 30 minutes, 60 minutes
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Result:Stimulated S1P1 phosphorylation in a time-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male albino Wistar rats (8-10 weeks old; 180-230 g) infected ocular endothelin-1 (ET-1)[2]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; daily; for 5 days
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Result:Visual evoked potentials (VEP) showed preserved visual function. Showed significantly higher retinal ganglion cells (RGCs) numbers.
化学情報
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CAS 番号 1094042-01-9
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性状 Solid
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分子量 409.48
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分子式 C23H27N3O4
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SMILES
CCOC1=CC=C(C2=NC(C3=CC=CC4=C3CCC4NCCO)=NO2)C=C1OCC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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PLoS Biol
Structural insights into subtype-specific agonist recognition by sphingosine-1-phosphate receptors. [Abstract]2026 Apr 10;24(4):e3003381. PMID: 41961881 -
Int Immunopharmacol
CD83 mediates the inhibitory effect of the S1PR1 agonist CYM5442 on LPS-induced M1 polarization of macrophages through the ERK-STAT-1 signaling pathway. [Abstract]2024 Oct 31;143(Pt 3):113526. PMID: 39486189 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
Hepatobiliary Pancreat Dis Int
Tripartite motif-containing 67 promotes progression of hepatocellular carcinoma by regulating MAPK signaling pathway. [Abstract]2026 Apr 27. PMID: 42106217 -
溶剤 & 溶解度
DMSO : 2.63 mg/mL (6.42 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gonzalez-Cabrera PJ, et al. Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like headgroup interactions. Mol Pharmacol. 2008 Nov;74(5):1308-18. [Content Brief]
[2]. Blanco R, et al. The S1P1 receptor-selective agonist CYM-5442 protects retinal ganglion cells in endothelin-1 induced retinal ganglion cell loss. Exp Eye Res. 2017 Nov;164:37-45. [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 | 2.4421 mL | 12.2106 mL | 24.4212 mL | 61.0530 mL |
| 5 mM | 0.4884 mL | 2.4421 mL | 4.8842 mL | 12.2106 mL |
CYM5442 関連分類
HY-10968 関連分類
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