Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rolapitant (SCH619734) hydrochloride 是一种高效选择性和具有口服活性的神经激肽 1 (NK1) 受体拮抗剂,Ki 值为 0.66 nM。Rolapitant hydrochloride (Rolapitant HCl) 不与 CYP3A4 产生互作。Rolapitant hydrochloride 在雪貂呕吐模型中显示出强效的中枢介导的止吐活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,780 | 现货 | ||
5 mg | ¥ 4,480 | 现货 | ||
10 mg | ¥ 6,380 | 现货 | ||
25 mg | ¥ 9,620 | 现货 | ||
50 mg | ¥ 12,900 | 现货 | ||
100 mg | ¥ 17,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 5,330 | 现货 |
产品描述 | Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a K i of 0.66 nM. Rolapitant hydrochloride (Rolapitant HCl) does not interact with CYP3A4. Rolapitant hydrochloride shows potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2]. |
体外活性 | In vitro studies indicate that rolapitant has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit [1]. Rolapitant (1-1000 nM) inhibits the GR-73632 (an NK1 receptor agonist)-induced calcium efflux with a concentration-dependent and competitive manner in CHO cells expressing the human NK1 receptor [1]. |
体内活性 | Rolapitant (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) reverses the GR-73632-induced foot-tapping response in Mongolian Gerbils [1]. Rolapitant (0.03-1 mg/kg; PO; single dosage; observed for 72 h) blocks acute emesis induced by both apomorphine and cisplatin in ferrets [1]. Animal Model: Female Mongolian Gerbils (30-60 g; anesthetized by inhalation of an oxygen:isofluorane mixture after 4 h PO or immediately after IV, then injected with 5 μl of 3 pmol solution of GR-73632 via ICV) [1] Dosage: 0.03, 0.1, 0.3 and 1 mg/kg for PO, 0.3 and 1 mg/kg for IV Administration: PO or IV, single dosage Result: Attenuated dose-dependently the GR-73632-induced foot-tapping response when administered PO 4 h before testing, with an ID 90 of 0.3 mg/kg, and the inhibition in foot tapping for at least 24 h. Blocked dose-dependently the foot tapping induced by GR-73632 when administered IV, with complete blockade observed at 1 mg/kg. Animal Model: Ferrets (treated with subcutaneous administration of 0.125 mg/kg apomorphine or intraperitoneal administration of 10 mg/kg cisplatin) [1] Dosage: 0.03, 0.1, 0.3 and 1 mg/kg Administration: PO; single dosage; observed for 72 h Result: Blocked dose-dependently acute emesis induced by both apomorphine and cisplatin in ferrets. Produced a robust decrease in retches and vomits in ferrets that was maintained throughout the 72 h observation period. Clinical efficacy of anti-emetics is highly correlated with efficacy in the ferret emesis model, suggesting rolapitant is a viable clinical candidate for this indication. |
别名 | Rolapitant HCl, 罗拉匹坦盐酸盐 |
分子量 | 536.94 |
分子式 | C25H27ClF6N2O2 |
CAS No. | 858102-79-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (93.12 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8624 mL | 9.312 mL | 18.6241 mL | 46.5601 mL |
5 mM | 0.3725 mL | 1.8624 mL | 3.7248 mL | 9.312 mL | |
10 mM | 0.1862 mL | 0.9312 mL | 1.8624 mL | 4.656 mL | |
20 mM | 0.0931 mL | 0.4656 mL | 0.9312 mL | 2.328 mL | |
50 mM | 0.0372 mL | 0.1862 mL | 0.3725 mL | 0.9312 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。
Rolapitant hydrochloride 858102-79-1 GPCR/G Protein Neuroscience Neurokinin receptor Rolapitant HCl Rolapitant Hydrochloride 罗拉匹坦盐酸盐 Inhibitor inhibitor inhibit