Pentagastrin - CAS:5534-95-2

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

目录号 : KM19126 CAS No. : 5534-95-2 纯度 : 98%

Data Sheet 产品使用指南

Pentagastrin (ICI-50123) 是胆囊收缩素 B (CCK_B) 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。

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生物活性

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

体外研究

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

体内研究

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 (pH_i) during acid challenge.

Animal Model:	Male Sprague-Dawley rats (approximately 200 g)
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 pH_i during acid challenge.

分子式

C₃₇H₄₉N₇O₉S

分子量

767.89

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。
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。