Pentagastrin(Synonyms: 五肽胃泌素; ICI-50123)

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Pentagastrin (Synonyms: 五肽胃泌素; ICI-50123) 纯度: 98.02%

Pentagastrin (ICI-50123) 是胆囊收缩素 B (CCKB) 受体的选择性激动剂,IC50 为 11 nM。可增强胃粘膜对酸的防御机制,并保护胃粘膜免受损伤。

Pentagastrin(Synonyms: 五肽胃泌素; ICI-50123)

Pentagastrin Chemical Structure

CAS No. : 5534-95-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥676 In-stock
5 mg ¥550 In-stock
10 mg ¥800 In-stock
25 mg ¥1600 In-stock
50 mg ¥2600 In-stock
100 mg ¥4400 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM[1]. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury[2].

IC50 & Target

IC50: 11 nM (CCKB receptor)[1]

体外研究
(In Vitro)

Cholecystokinin receptors on GH3 rat anterior pituitary cells have been characterised using radioligand binding and Ca2+ mobilisation. Competition curve with Pentagastrin (IC50 of 25 nM) is consistent with a population predominantly of CCKB receptors. The selective CCKB receptor agonist, Pentagastrin, (0.1 nM-100 μM) dose dependently increased intracellular Ca2+ with a maximal increase of 2.77-fold. Binding of 50 pM [125I]BHCCK to GH 3 cells is dose dependently inhibited by Pentagastrin IC50 of 45 nM. Response to a submaximal dose of the CCKB receptor agonist Pentagastrin (100 nM) was dose dependently blocked by the CCKB receptor antagonist L-365,260[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Pentagastrin (80 µg/kg/h; intravenous injection; male Sprague-Dawley rats) treatment protects rat gastric mucosa from acidified aspirin injury. Pentagastrin induces a hyperaemic response to luminal acid challenge, increases mucus gel thickness, and elevates intracellular pH (pHi) during acid challenge[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (approximately 200 g)[2]
Dosage: 80 µg/kg/h
Administration: Intravenous injection
Result: Protected rat gastric mucosa from acidified aspirin injury. Induced a hyperaemic response to luminal acid challenge, increased mucus gel thickness, and elevated pHi during acid challenge.

分子量

767.89

Formula

C37H49N7O9S

CAS 号

5534-95-2

中文名称

五肽胃泌素;五肽胃必素;五肽促胃液素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light

Powder -80°C 2 years
-20°C 1 year

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

溶解性数据
In Vitro: 

DMSO : ≥ 34 mg/mL (44.28 mM)

H2O : 1 mg/mL (1.30 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3023 mL 6.5113 mL 13.0227 mL
5 mM 0.2605 mL 1.3023 mL 2.6045 mL
10 mM 0.1302 mL 0.6511 mL 1.3023 mL

*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.71 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Smith AJ, et al. Characterisation of CCKB receptors on GH3 pituitary cells: receptor activation is linked to Ca2+ mobilisation. Eur J Pharmacol. 1994 Apr 15;267(2):215-23.

    [2]. Tanaka S, et al. Pentagastrin gastroprotection against acid is related to H2 receptor activation but not acid secretion. Gut. 1998 Sep;43(3):334-41.

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