Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sarpogrelate hydrochloride (MCI-9042) 是一种选择性5-HT2R 拮抗剂,可用于研究与血栓形成有关的血管疾病,对 5-HT2A、5-HT2B 和 5-HT2C 受体的pKi 值分别为 8.52、6.57 和 7.43。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 169 | 现货 | ||
5 mg | ¥ 383 | 现货 | ||
10 mg | ¥ 617 | 现货 | ||
25 mg | ¥ 1,090 | 现货 | ||
50 mg | ¥ 1,620 | 现货 | ||
100 mg | ¥ 2,420 | 现货 | ||
500 mg | ¥ 5,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 433 | 现货 |
产品描述 | Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD. |
靶点活性 | 5-HT2A:8.39 nM(Ki) |
别名 | 盐酸沙格雷酯, MCI-9042 |
分子量 | 465.97 |
分子式 | C24H32ClNO6 |
CAS No. | 135159-51-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 46.6 mg/mL(100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1461 mL | 10.7303 mL | 21.4606 mL | 53.6515 mL |
5 mM | 0.4292 mL | 2.1461 mL | 4.2921 mL | 10.7303 mL | |
10 mM | 0.2146 mL | 1.073 mL | 2.1461 mL | 5.3652 mL | |
20 mM | 0.1073 mL | 0.5365 mL | 1.073 mL | 2.6826 mL | |
50 mM | 0.0429 mL | 0.2146 mL | 0.4292 mL | 1.073 mL | |
100 mM | 0.0215 mL | 0.1073 mL | 0.2146 mL | 0.5365 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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