Proglumide sodium

立即咨询

Proglumide sodium

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

99247-33-3

丙谷胺钠；蒙胃顿钠

Proglumide sodium 是一种非肽和口服活性胆囊收缩素(CCK)-A/B受体拮抗剂。Proglumide sodium 选择性阻断CCK在中枢神经系统中的作用。Proglumide sodium 具有抑制胃分泌和保护胃十二指肠粘膜的能力，还具有抗癫痫和抗氧化活性。

生物活性

Proglumide sodium is a nonpeptide and orally activecholecystokinin (CCK)-A/B receptorsantagonist. Proglumide sodium selective blocksCCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities^[1]^[2]^[3]^[4]^[5].

IC₅₀& Target

Cholecystokinin (CCK)-A/B receptors^[1]^[2]

体外研究
(In Vitro)

In an in vitro study, Proglumide at concentrations between 0.3-10 mM inhibits CCK-stimulated amylase release dose-dependently, while Proglumide does not influence the basal amylase release at concentrations between 0-3 mM. Dose-response curves to CCK for amylase release shifted to the right with increase in Proglumide concentration. This inhibition by Proglumide is reversible. In addition, the effect of Proglumide is selective for CCK and its related peptide^[2].
The incubation of HT29 cells with Proglumide significantly reduces the [³H]-thymidine incorporation to HT29 cells in a dose-dependent manner, with an IC₅₀of 6.5 mM. Proglumide reduces in a dose-dependent manner the percentage of necrosis with a parallel increase of apoptosis up to 70%^[3].

体内研究
(In Vivo)

Proglumide (250-750 mg/kg; intraperitoneal injection; adult male Sprague Dawley rats) treatment is significantly effective in ameliorating the seizure activities, cognitive dysfunctions, and cerebral oxidative stress^[1].

Animal Model:	Adult male Sprague Dawley rats (200-250 g; 2 months old) are induced status epilepticus (SE)^[1]
Dosage:	250 mg/kg, 500 mg/kg, and 750 mg/kg
Administration:	Intraperitoneal injection
Result:	Dose-dependently and significantly increased the latencies to seizure and SE. Significantly and dose-dependently attenuated Li-PC (SE) induced increase in thiobarbituric acid (TBARS) and catalase (CAT), attenuated Li-Pc induced decrease in SOD, and attenuated depletion of GSH and glutathione-S transferase (GST) in the hippocampus and striatum.

Clinical Trial

分子量

356.39

性状

Solid

Formula

C₁₈H₂₅N₂NaO₄

CAS 号

99247-33-3

中文名称

丙谷胺钠；蒙胃顿钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

H₂O : 100 mg/mL(280.59 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.8059 mL	14.0296 mL	28.0591 mL
5 mM	0.5612 mL	2.8059 mL	5.6118 mL
10 mM	0.2806 mL	1.4030 mL	2.8059 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℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： PBS
Solubility: 100 mg/mL (280.59 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。