CYM5442 MedChemExpress (MCE)

Product Name	CYM 5442 HCL
Synonyms	CYM 5442 HCL
CAS	1783987-80-3
EINECS
Chemical Formula	C23H28ClN3O4
Molecular Weight	445.94
inchi
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Descriptions	CYM5442 hydrochloride CYM5442 hydrochloride MedChemExpress (MCE) HY-10968A 1783987-80-3 Please store the product under the recommended conditions in the Certificate of Analysis. Room temperature in continental US Descriptions CYM5442 hydrochloride CYM5442 hydrochloride MedChemExpress (MCE) HY-10968A 1783987-80-3 Please store the product under the recommended conditions in the Certificate of Analysis. Room temperature in continental US may vary elsewhere. 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). 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]. CYM5442 (1 mg/kg intraperitoneal injection daily for 5 days adult male albino Wistar rats) treatment shows preserved visual function of visual evoked potentials (VEP). Retinal nerve fiber layer (RNFL) is significantly thicker in the CYM treated-animals compared to the vehicle[2]. EC50: 1.35 nM (Sphingosine 1-phosphate (S1P1) receptor)[1] In Vitro 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. 0 --> CYM5442 hydrochloride Related Antibodies Western Blot Analysis[1] Cell Line: HEK293 cells stably expressing S1P1 fused to GFP on the carboxy-terminus \| \| \| \| \| \| \| \| \| \| [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]
Supplier Website	https://www.medchemexpress.com/cym5442-hydrochloride.html
Last Update	2025-05-21 16:50:25

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