产品
编 号:F131722
分子式:C24H32ClNO6
分子量:465.97
产品类型
结构图
CAS No: 135159-51-2
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产品详情
生物活性:
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
体内研究:
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.
体外研究:
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.