| Bioactivity | Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model[1][2]. |
| Invitro | Rolapitant hydrochloride hydrate 对人类 NK2 和 NK3 亚型的选择性超过 1000 倍，并且对人类、豚鼠、沙鼠和猴子 NK1 受体的亲和力优于大鼠、小鼠和兔[1].Rolapitant hydrochloride hydrate (1-1000 nM) 在表达人 NK1 受体的 CHO 细胞中以浓度依赖性和竞争性方式抑制 GR-73632 (一种 NK1 受体激动剂) 诱导的钙流出[1]。 |
| In Vivo | Rolapitant hydrochloride hydrate (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) 减弱蒙古沙鼠中 GR-73632 (HY-P1192) 诱导的足部敲击反应[1]。Rolapitant hydrochloride hydrate (0.03-1 mg/kg; PO; single dosage; observed for 72 h) 阻断雪貂中由阿扑吗啡和 cisplatin (HY-17394) 引起的急性呕吐[1]。 Animal Model: |
| Name | Rolapitant hydrochloride hydrate |
| CAS | 914462-92-3 |
| Formula | C25H29ClF6N2O3 |
| Molar Mass | 554.95 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. [2]. Rapoport B, et al. Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC). Support Care Cancer. 2015 Nov;23(11):3281-8. |
Rolapitant hydrochloride hydrate
CAS: 914462-92-3 F: C25H29ClF6N2O3 W: 554.95
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.