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Laropiprant (MK-0524) 是 DP receptor 的选择性拮抗剂,Ki 为 0.57 nM,对 TP 受体的 Ki 为 2.95 nM。
Laropiprant (MK-0524) 是 DP receptor 的选择性拮抗剂,Ki 为 0.57 nM,对 TP 受体的 Ki 为 2.95 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 223 | 现货 | |
5 mg | ¥ 491 | 现货 | |
10 mg | ¥ 738 | 现货 | |
25 mg | ¥ 1,390 | 现货 | |
50 mg | ¥ 2,210 | 现货 | |
100 mg | ¥ 3,290 | 现货 | |
200 mg | ¥ 4,520 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 530 | 现货 |
产品描述 | Laropiprant (MK-0524) is a potent and selective antagonist of prostaglandin D2 (PGD2) receptor (DP) such as and DP/DP1 receptor(Ki = 0.57 nM) and TP Receptor(Ki = 2.95 nM). |
靶点活性 | TP receptor:2.95 nM (ki), DP/DP1 receptor:0.57 nM (ki) |
体外活性 | Laropiprant blocks DP receptor-dependent enhance in VASP phosphorylation, as well as inhibition of P-selectin expression, GPIIb/IIIa activation, and in vitro thrombus formation. Laropiprant antagonizes the increased platelet aggregation by TP and EP3 receptor activation. Laropiprant (1 μM) induces a significant inhibition of the aggregation but still counteracts the pronounced inhibition caused by PGD2 (30 nM) and BW245c (3 nM). Laropiprant (10 μM) and niacin inhibit in vitro thrombus formation[2]. |
别名 | MK-0524 |
分子量 | 435.9 |
分子式 | C21H19ClFNO4S |
CAS No. | 571170-77-9 |
Smiles | CS(=O)(=O)c1cc(F)cc2c3CC[C@H](CC(O)=O)c3n(Cc3ccc(Cl)cc3)c12 |
密度 | 1.486 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (229.41 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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