2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Rolapitant hydrochloride

Rolapitant hydrochloride  (Synonyms: 罗拉匹坦盐酸盐; SCH619734 hydrochloride)

目录号: HY-14751A
产品使用指南

摩尔计算器

Rolapitant (SCH619734) hydrochloride 是一种长效且具有选择性和口服活性的神经激肽 1 (NK1) 受体拮抗剂，Ki 值为 0.66 nM。Rolapitant hydrochloride 不与 CYP3A4 产生互作。Rolapitant hydrochloride 在雪貂呕吐模型中显示出强效的止吐活性。

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Rolapitant hydrochloride Chemical Structure

Rolapitant hydrochloride Chemical Structure

CAS No. : 858102-79-1

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Rolapitant hydrochloride 的其他形式现货产品:

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Rolapitant hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model[1][2].

IC50 & Target[1]

human NK1

0.66 (Ki)

gerbil NK1

0.13 (Ki)

guinea pig NK1

0.72 (Ki)

monkey NK1

2.5 (Ki)

rabbit NK1

31.7 (Ki)

rat NK1

78.6 (Ki)

mouse NK1

60.4 (Ki)

体外研究
(In Vitro)

Rolapitant has high selectivity over the human NK2 and NK3 subtypes of more than 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Rolapitant hydrochloride 相关抗体:
体内研究
(In Vivo)

Rolapitant (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) attenuates 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 ID90 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 Trial
分子量

536.94

Formula

C25H27ClF6N2O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Rolapitant hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rolapitant858102-79-1SCH619734SCH 619734SCH-619734Neurokinin ReceptorNK receptorTachykinin receptorlong-actingorally activeanti-emeticemesisferretMongolian Gerbilsfoot tappingretchesvomitsInhibitorinhibitorinhibit

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