Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Selexipag (ACT-293987) 是前列环素受体激动剂,可引起肺血管舒张,用于治疗肺动脉高压。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 398 | 现货 | ||
5 mg | ¥ 597 | 现货 | ||
10 mg | ¥ 984 | 现货 | ||
25 mg | ¥ 1,630 | 现货 | ||
50 mg | ¥ 2,337 | 现货 | ||
100 mg | ¥ 3,747 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 697 | 现货 |
产品描述 | Selexipag (ACT-293987)(NS-304) is prostacyclin receptor agonist that causes vasodilation in pulmonary vasculature and is used in the therapy of pulmonary arterial hypertension (PAH). |
体外活性 | NS-304 is an orally available and long-acting IP receptor agonist prodrug, and its active form, MRE-269, is highly selective for the IP receptor. NS-304 inhibits the binding of [3H]Iloprost to the human and rat IP receptors in a concentration-dependent manner. The Ki is 260 nM for the human IP receptor and 2100 nM for the rat IP receptor. The intracellular cAMP levels in hIP-CHO cells are increased in a concentration-dependent manner by treatment with NS-304 with EC50 of 177 nM. NS-304 also inhibits platelet aggregation in humans and monkeys with IC50 values of 5.5 and 3.4 μM, respectively, but it shows no inhibition in dogs (IC50 of >100 μM)[1]. |
体内活性 | The Cmax of MRE-269 after oral administration of NS-304 is 1.1 μg/mL in rats and 9.0 μg/mL in dogs. NS-304 at 1 or 3 mg/kg increases FSBF in anesthetized rats for more than 4 h after intraduodenal administration in a dose-dependent manner. In particular, NS-304 at 3 mg/kg causes a sustained increase in FSBF and exhibits a maximal increase of 93% in FSBF 1 h after administration[1]. |
细胞实验 | NS-304 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. CHO cells expressing the human IP receptor (hIP-CHO cells) are seeded at 1×105 cells/well in a 24-well plate and cultured for 48 h. The cells are washed with Dulbecco's phosphate-buffered saline without divalent cations, preincubated in the medium for 1 h at 37°C, and then incubated for 15 min at 37°C with medium containing each drug in the presence of 500 μM 3-isobutyl-1-methylxanthine. The medium is removed, and perchloric acid solution is added to terminate the reaction. Intracellular cAMP levels are measured by enzymelinked immunosorbent assay[1]. |
别名 | NS-304, ACT-293987, 赛乐西帕, Uptravi |
分子量 | 496.62 |
分子式 | C26H32N4O4S |
CAS No. | 475086-01-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 49.7 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 | 2.0136 mL | 10.0681 mL | 20.1361 mL | 50.3403 mL |
5 mM | 0.4027 mL | 2.0136 mL | 4.0272 mL | 10.0681 mL | |
10 mM | 0.2014 mL | 1.0068 mL | 2.0136 mL | 5.034 mL | |
20 mM | 0.1007 mL | 0.5034 mL | 1.0068 mL | 2.517 mL | |
50 mM | 0.0403 mL | 0.2014 mL | 0.4027 mL | 1.0068 mL | |
100 mM | 0.0201 mL | 0.1007 mL | 0.2014 mL | 0.5034 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。
Selexipag 475086-01-2 GPCR/G Protein Immunology/Inflammation Others Prostaglandin Receptor NS 304 NS-304 ACT 293987 ACT-293987 赛乐西帕 Uptravi Inhibitor inhibit NS304 ACT293987 inhibitor