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

Rolapitant hydrochloride hydrate  (Synonyms: SCH619734 hydrochloride hydrate)

目錄號: HY-16436 純度: 98.25%
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Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) 是一種長效且具有選擇性和口服活性的神經激肽 1 (NK1) 受體拮抗劑，Ki 值為 0.66 nM。Rolapitant hydrochloride hydrate 不與 CYP3A4 產生互作。Rolapitant hydrochloride hydrate 在雪貂嘔吐模型中顯示出強效的止吐活性。

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Rolapitant hydrochloride hydrate Chemical Structure

Rolapitant hydrochloride hydrate Chemical Structure

CAS No. : 914462-92-3

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥733
In-stock
5 mg ￥600
In-stock
10 mg ￥960
In-stock
25 mg ￥1950
In-stock
50 mg ￥3200
In-stock
100 mg ￥5200
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200 mg   詢價  
500 mg   詢價  

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Other Forms of Rolapitant hydrochloride hydrate:

查看 Neurokinin Receptor 亞型特異性產品:

  • 生物活性

  • 純度 & 產品資料

  • 參考文獻

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)

體外研究
(In Vitro)

Rolapitant hydrochloride hydrate 對人類 NK2 和 NK3 亞型的選擇性超過 1000 倍，并且對人類、豚鼠、沙鼠和猴子 NK1 受體的親和力優(yōu)于大鼠、小鼠和兔[1].
Rolapitant hydrochloride hydrate (1-1000 nM) 在表達人 NK1 受體的 CHO 細胞中以濃度依賴性和競爭性方式抑制 GR-73632 (一種 NK1 受體激動劑) 誘導的鈣流出[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內研究
(In Vivo)

Rolapitant hydrochloride hydrate (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) 減弱蒙古沙鼠中 GR-73632 (HY-P1192) 誘導的足部敲擊反應[1]。
Rolapitant hydrochloride hydrate (0.03-1 mg/kg; PO; single dosage; observed for 72 h) 阻斷雪貂中由阿撲嗎啡和 cisplatin (HY-17394) 引起的急性嘔吐[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 號
性狀

固體

顏色

White to off-white

運輸條件

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

4°C, protect from light

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

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 250 mg/mL (450.49 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質量 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
查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產品資料
參考文獻

完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 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.

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產品名稱：
Rolapitant hydrochloride hydrate
目錄號：
HY-16436
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