| 中文名称 | 盐酸沙格雷酯 |
| 英文名称 | Sarpogrelate hydrochloride |
| CAS号 | 135159-51-2 |
| 分子式 | C24H32ClNO6 |
| 分子量 | 465.96698 |
| EINECS号 | 663-199-9 |
| 熔点 | 145-148°C |
| 溶解度 | 去离子水:≥5mg/mL |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
| 危险品标志 | Xn,N |
| 危险类别码 | 22-50/53 |
| 安全说明 | 60-61 |
| 危险品运输编号 | UN 3077 9 / PGIII |
| WGK Germany | 3 |
| 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. |