| Bioactivity | CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM[1]. | |||||||||
| Target | EC50: 56 nM (S1P4-R), 2100 nM (S1P5-R) | |||||||||
| Invitro | The disclosed lead molecule CYM50308 (Compound 24f) displays low nanomolar S1P4-R agonist activity and exquisite selectivity over the other S1P-Rs subtypes. Noteworthy, CYM50308 provides a valuable pharmacological tool to explore the effects of the S1P4-R signaling cascade and elucidate the molecular basis of the in vivo receptor function[1]. | |||||||||
| Name | CYM50308 | |||||||||
| CAS | 1345858-76-5 | |||||||||
| Formula | C20H21F2N3O2S | |||||||||
| Molar Mass | 405.46 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Urbano M, et al. Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6739-45. |
CYM50308
CAS: 1345858-76-5 F: C20H21F2N3O2S W: 405.46
CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC
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