CYM 5541

Research use only, not for human use.

CYM-5541 is a selective and allosteric S1P3 receptor agonist.

CYM-5541 is a selective, allosteric agonist of S1P3 (EC50 = 72-132 nM). Sphingosine 1-phosphate (S1P) is a lysophospholipid signaling molecule that regulates important biological functions, including lymphocyte trafficking and vascular development, by activating G protein-coupled receptors for S1P, namely, S1P(1) through S1P(5).

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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CYM-5541 | CYM 5541 | CYM5541

Metabolic Enzyme/Protease

NAMPT

S1P3

Cardiovascular Disease

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945128-26-7

316.44

C19H28N2O2

>98% (HPLC)

DMSO : ≥ 39 mg/mL; 123.25 mM

C1CCC(CC1)N(C1CCCCC1)C(=O)c1noc(c1)C1CC1

N,N-dicyclohexyl-5-cyclopropyl-3-isoxazolecarboxamide

(-20℃)

With Ice Pack

≥ 2 years