CYM5442 hydrochloride

CAS: 1783987-80-3 F: C23H28ClN3O4 W: 445.94

CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist wi

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Bioactivity	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)[1][2].
Target	EC50: 1.35 nM (Sphingosine 1-phosphate (S1P1) receptor)
Invitro	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]. Western Blot Analysis[1] Cell Line:
In Vivo	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]. Animal Model:
Name	CYM5442 hydrochloride
CAS	1783987-80-3
Formula	C23H28ClN3O4
Molar Mass	445.94
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.