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CYM-5541

CAS No. : 945128-26-7

產(chǎn)品活性：CYM-5541 (ML249) is an selective and allosteric S1P₃ receptor agonist with an EC₅₀ between 72 and 132 nM.

研究領(lǐng)域：GPCR/G Protein

作用靶點：LPL Receptor

In Vitro: CYM-5541 is a full agonist, able to reach the maximum level of ERK phosphorylation that is observed with S1P. CYM-5541 has an EC₅₀ of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes: S1P1 EC₅₀>10 μM, S1P2 EC₅₀>50 μM, S1P4 EC₅₀>50 μM, and S1P5 EC₅₀>25 μM. CYM-5541 also shows selectivity over a large panel of protein targets, with no significant activities, in the Ricerca profiling panel of 55 GPCRs, ion channels, and transporters. CYM-5541 allowed us to identify an allosteric site where F263 is a key gate-keeper residue for its affinity and efficacy. The novel allosteric hydrophobic pocket may account for the S1P3 selectivity of CYM-5541.

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