Sarpogrelate hydrochloride

Research use only, not for human use.

A potent, specific 5HT2 receptor antagonist with Ki of 8.39 nM for 5-HT2A; also shows binding affinity for 5-HT2B.

A potent, specific 5HT2 receptor antagonist with Ki of 8.39 nM for 5-HT2A; also shows binding affinity for 5-HT2B; displays selectivity over 5-HT1-like, 5-HT3, beta, H1, H2 and M3; blocks serotonin-induced platelet aggregation.Heart Failure Approved(In Vitro):Sarpogrelate is selective for 5-HT2 (pKi=7.54) over 5-HT1 (pKi=4.58), α1-, α2-, and β-adrenergic (pKi=3.17-6.19), and muscarinic receptors (pKi=4.39).Sarpogrelate (10 μM) significantly reduces the number of platelet-rich plasma (PRP)-induced THP-1 cell that adheres to human umbilical vein endothelial cells (HUVECs).Sarpogrelate (10 μM) significantly reduces the expression of PRP-induced E-selectin in HUVECs.(In Vivo):Sarpogrelate (5 mg/kg; i.p. daily for 4 weeks) inhibits HFFD-induced obesity and decreases leukocyte-endothelial interactions in mice.

Sarpogrelate is selective for 5-HT2 (pKi=7.54) over 5-HT1 (pKi=4.58), α1-, α2-, and β-adrenergic (pKi=3.17-6.19), and muscarinic receptors (pKi=4.39).Sarpogrelate (10 μM) significantly reduces the number of platelet-rich plasma (PRP)-induced THP-1 cell that adheres to human umbilical vein endothelial cells (HUVECs).Sarpogrelate (10 μM) significantly reduces the expression of PRP-induced E-selectin in HUVECs.

Sarpogrelate (5 mg/kg; i.p. daily for 4 weeks) inhibits HFFD-induced obesity and decreases leukocyte-endothelial interactions in mice. Animal Model:Male C57BL/6 mice (7 weeks old) are fed normal chow (NC) or a high-fat diet with 30% fructose in the drinking water (HFFD)Dosage:5 mg/kg Administration:I.p. daily for 4 weeks Result:Prevented the HFFD-induced increases of the body weight, visceral fat weight, and serum monocyte chemoattractant protein-1 levels.Decreased leukocyte-endothelial interactions and serum monocyte chemoattractant protein-1 (MCP-1) level.

MCI 9042 | MCI9042 | MCI-9042

Endocrinology/Hormones

5-HT Receptor

5-HT Receptor

Cardiovascular Disease

——

135159-51-2

465.967

C24H32ClNO6

>98% (HPLC)

DMSO: ≥ 62 mg/mL

CN(C)CC(COC1=CC=CC=C1CCC2=CC(=CC=C2)OC)OC(=O)CCC(=O)O.Cl

Butanedioic acid, 1-[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl]ethyl] ester, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years