盐酸沙格雷酯
中文名称 | 盐酸沙格雷酯 |
---|---|
中文同义词 | 盐酸沙格雷酯;沙格雷酯盐酸盐;(+/-)-2-(二甲胺基)-1-{[2-(3-甲氧基苯基)苯氧基]甲基}乙基丁二酸单酯盐酸盐;盐酸沙普酯;沙格雷酯-D3盐酸;SARPOGRELATE盐酸盐;1-2-(二甲胺基)-1-[[2-[2-(3-甲氧基苯基)乙基]苯氧基]甲基]乙基]丁二酸单酯盐酸盐;(+/-)-2-(二甲胺基)-1-{[2-(3-甲氧基苯基)苯氧基]甲基}乙基丁二酸单酯盐酸盐 |
英文名称 | Sarpogrelate hydrochloride |
英文同义词 | Sarpogrelate-D3 HCl;Anplag;Butanedioic acid, mono[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl]ethyl] ester, hydrochloride (9CI);Butanedioic acid, mono[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl]ethyl] ester, hydrochloride, (+-)-;MCI 9042;4-[1-(dimethylamino)-3-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]propan-2-yl]oxy-4-oxobutanoic acid hydrochloride;4-[1-(dimethylamino)-3-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]propan-2-yl]oxy-4-oxo-butanoic acid hydrochloride;4-[1-(dimethylaminomethyl)-2-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]ethoxy]-4-keto-butyric acid hydrochloride |
CAS号 | 135159-51-2 |
分子式 | C24H32ClNO6 |
分子量 | 465.96698 |
EINECS号 | 663-199-9 |
相关类别 | 医药中间体;沙格雷酯;医药原料;医药原料药;合成;中间体;原料;Amines;Aromatics;Intermediates & Fine Chemicals;Pharmaceuticals;fang;strong recommend |
Mol文件 | 135159-51-2.mol |
结构式 |
盐酸沙格雷酯 性质
熔点 | 145-148°C |
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储存条件 | Inert atmosphere,2-8°C |
溶解度 | 去离子水:≥5mg/mL |
形态 | 固体 |
颜色 | 白色至米白色 |
InChIKey | POQBIDFFYCYHOB-UHFFFAOYSA-N |
CAS 数据库 | 135159-51-2(CAS DataBase Reference) |
Target | Value |
5-HT2A
(Cell-free) | 0.2 nM(Kd) |
5-HT2C
(Cell-free) | 1.1 nM(Kd) |
5-HT2B
(Cell-free) | 2.1 nM(Ki) |
5-HT2B
(Cell-free) | 2.1 nM(Kd) |
Sarpogrelate is selective for 5-HT
2
(pK
i
=7.54) over 5-HT
1
(pK
i
=4.58), α
1
-, α
2
-, and β-adrenergic (pK
i
=3.17-6.19), and muscarinic receptors (pK
i
=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. |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | 46191 | 盐酸沙格雷酯, 98% Sarpogrelate hydrochloride, 98% | 135159-51-2 | 250mg | 1604元 |
2024/08/19 | 46191 | 盐酸沙格雷酯, 98% Sarpogrelate hydrochloride, 98% | 135159-51-2 | 1g | 5272元 |