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CAS No. : 945128-26-7
MCE 国际站:CYM-5541
产品活性:CYM-5541 (ML249)是选择性的S1P3受体变构激动剂,EC50值在72至132 nM之间。
研究领域:GPCR/G Protein
作用靶点: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.
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Anti-Cardiovascular Disease Compound Library | Targeted Diversity Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | BMS-986020 sodium | ONO-0300302 | BMS-986278 | NAEPA | Sphingosine-1-phosphate-d7 | S1P1 agonist III | S1PR1 modulator 1 | LPA2 antagonist 2 | Radioprotectin-1 | S1PR1 agonist 1 | TC-SP 14 | CYM50358 | W146 | Udifitimod | CRT0273750 | Ki16425 | ONO-9780307 | CS-2100 | Fingolimod phosphate-d4 | CAY10444 | ONO-0740556 | NIBR0213 | CYM50260 | ASP-4058 | FTY720 (S)-Phosphate | Sonepcizumab | TAK-615 | GSK2018682 | Mocravimod hydrochloride
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