| 名称 | Rolapitant hydrochloride |
| 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, which does not interact with CYP3A4 and demonstrates 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, administered orally (0.03-1 mg/kg) or intravenously (0.3-1 mg/kg) as a single dose, effectively mitigates the GR-73632-induced foot-tapping in Mongolian Gerbils and prevents acute emesis triggered by apomorphine and cisplatin in ferrets, with observations lasting up to 72 hours. In the Mongolian Gerbil model, the compound, when given orally, significantly reduces the foot-tapping response, achieving an ID90 at 0.3 mg/kg and maintaining inhibition for over 24 hours. Intravenous administration resulted in a complete cessation of foot-tapping at a dose of 1 mg/kg. In ferrets, rolapitant dose-dependently inhibits vomiting and retching induced by both emetic agents over a 72-hour period, illustrating its potential as an effective clinical antiemetic. This aligns with the ferret emesis model's predictive value for clinical antiemetic efficacy, endorsing rolapitant as a promising candidate for this purpose. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (93.12 mM)
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| 关键字 | Rolapitant hydrochloride | Rolapitant Hydrochloride |
| 相关产品 | Rolapitant | Ezlopitant | (R)-CJ 11974 | N-Acetyl-L-tryptophan | Netupitant | Aprepitant | Befetupitant | Vofopitant | Fosaprepitant dimeglumine | Maropitant |
| 相关库 | 疼痛相关化合物库 | 经典已知活性库 | 膜蛋白靶向化合物库 | EMA 上市药物库 | 药物功能重定位化合物库 | 抑制剂库 | 抗癌上市药物库 | 已知活性化合物库 | GPCR靶点分子库 | 抗癌药物库 |
United States
