CYM5442 is a potent, highly-selective and orally activesphingosine 1-phosphate (S1P1) receptoragonist with anEC₅₀of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activatesS1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS)^[1][2].

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 EC₅₀of 46 nM. The R120 for alanine (R120A) mutant is still able to maintain p42/p44-MAPK activity when incubated with CYM5442 (EC₅₀of 67 nM). Activation of p42/p44-MAPK by CYM5442 in E121A S1P1 cells is concentration dependent, with a mean EC₅₀value 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].

409.48

Solid

C₂₃H₂₇N₃O₄

1094042-01-9

Room temperature in continental US; may vary elsewhere.

DMSO : 2.63 mg/mL(6.42 mM;Need ultrasonic)

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