Sarpogrelate (hydrochloride)

Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells). It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), alpha1-, alpha2-, and beta-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM). In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT (Cay-14332) with collagen, and 5-HT with ADP (Cay-16778, IC50s = 57.7, 0.56, and 22.7 µM, respectively). In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day. Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.Formal Name: butanedioic acid, 1-[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl]ethyl] ester, monohydrochloride. CAS Number: 135159-51-2. Synonyms: MCI-9042. Molecular Formula: C24H31NO6 . HCl. Formula Weight: 466.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMSO: 33 mg/ml, PBS (pH 7.2): 0.33 mg/ml. SMILES: COC1=CC=CC(CCC2=CC=CC=C2OCC(OC(CCC(O)=O)=O)CN(C)C)=C1.Cl. InChi Code: InChI=1S/C24H31NO6.ClH/c1-25(2)16-21(31-24(28)14-13-23(26)27)17-30-22-10-5-4-8-19(22)12-11-18-7-6-9-20(15-18)29-3,/h4-10,15,21H,11-14,16-17H2,1-3H3,(H,26,27),1H. InChi Key: POQBIDFFYCYHOB-UHFFFAOYSA-N.