CYM5442 hydrochloride
Based on 5 publication(s) in Google Scholar
CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride can easily penetrate the central nervous system (CNS).
For research use only. We do not sell to patients.
- CAS No.: 1783987-80-3
- Formula: C23H28ClN3O4
- Molecular Weight:445.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CYM5442 hydrochloride
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Biological Activity
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 CYM-5442 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.
Chemical Information
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CAS No. 1783987-80-3
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Molecular Weight 445.94
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Formula C23H28ClN3O4
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SMILES
CCOC1=CC=C(C2=NC(C3=CC=CC4=C3CCC4NCCO)=NO2)C=C1OCC.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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 -
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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