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

Rolapitant hydrochloride hydrate  (Synonyms: SCH619734 hydrochloride hydrate)

目录号: HY-16436 纯度: 98.25%
COA 产品使用指南

摩尔计算器

Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) 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 hydrate 不与 CYP3A4 产生互作。Rolapitant hydrochloride hydrate 在雪貂呕吐模型中显示出强效的止吐活性。

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Rolapitant hydrochloride hydrate Chemical Structure

Rolapitant hydrochloride hydrate Chemical Structure

CAS No. : 914462-92-3

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规格 价格 是否有货 数量
5 mg ￥600
In-stock
10 mg ￥960
In-stock
25 mg ￥1950
In-stock
50 mg ￥3200
In-stock
100 mg ￥5200
In-stock
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500 mg   询价  

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Customer Review

Other Forms of Rolapitant hydrochloride hydrate:

Rolapitant hydrochloride hydrate 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 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].

IC50 & Target[1]

human NK1

0.66 nM (Ki)

gerbil NK1

0.13 nM (Ki)

guinea pig NK1

0.72 nM (Ki)

monkey NK1

2.5 nM (Ki)

rabbit NK1

31.7 nM (Ki)

rat NK1

78.6 nM (Ki)

mouse NK1

60.4 nM (Ki)

体外研究
(In Vitro)

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]。

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

Rolapitant hydrochloride hydrate 相关抗体:
体内研究
(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]。

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

554.95

Formula

C25H29ClF6N2O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 250 mg/mL (450.49 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8020 mL 9.0098 mL 18.0196 mL
5 mM 0.3604 mL 1.8020 mL 3.6039 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Rolapitant hydrochloride hydrate 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8020 mL 9.0098 mL 18.0196 mL 45.0491 mL
5 mM 0.3604 mL 1.8020 mL 3.6039 mL 9.0098 mL
10 mM 0.1802 mL 0.9010 mL 1.8020 mL 4.5049 mL
15 mM 0.1201 mL 0.6007 mL 1.2013 mL 3.0033 mL
20 mM 0.0901 mL 0.4505 mL 0.9010 mL 2.2525 mL
25 mM 0.0721 mL 0.3604 mL 0.7208 mL 1.8020 mL
30 mM 0.0601 mL 0.3003 mL 0.6007 mL 1.5016 mL
40 mM 0.0450 mL 0.2252 mL 0.4505 mL 1.1262 mL
50 mM 0.0360 mL 0.1802 mL 0.3604 mL 0.9010 mL
60 mM 0.0300 mL 0.1502 mL 0.3003 mL 0.7508 mL
80 mM 0.0225 mL 0.1126 mL 0.2252 mL 0.5631 mL
100 mM 0.0180 mL 0.0901 mL 0.1802 mL 0.4505 mL
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:

Rolapitant hydrochloride914462-92-3SCH619734 hydrochlorideNeurokinin ReceptorNK receptorTachykinin receptorlong-actingorally activeanti-emeticemesisferretMongolian Gerbilsfoot tappingretchesvomitsInhibitorinhibitorinhibit

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目录号：
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