Proglumide sodium(Synonyms: 丙谷胺钠；蒙胃顿钠)

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Proglumide sodium (Synonyms: 丙谷胺钠；蒙胃顿钠) 纯度: 99.63%

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。

Proglumide sodium(Synonyms: 丙谷胺钠；蒙胃顿钠)

Proglumide sodium Chemical Structure

CAS No. : 99247-33-3

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10 mM * 1 mL in Water ￥660 In-stock
50 mg ￥600 In-stock
100 mg ￥1100 In-stock
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生物活性

Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’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 IC50 of 6.5 mM. Proglumide reduces in a dose-dependent manner the percentage of necrosis with a parallel increase of apoptosis up to 70%[3].

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)

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].

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: 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

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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-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。
参考文献

  • [1]. Ahmad M, et al. The effects of quinacrine, proglumide, and pentoxifylline on seizure activity, cognitive deficit, and oxidative stress in rat lithium-pilocarpine model of status epilepticus. Oxid Med Cell Longev. 2014;2014:630509.

    [2]. Iwamoto Y, et al. In vitro and in vivo effect of proglumide on cholecystokinin-stimulated amylase release in mouse pancreatic acini. Gastroenterol Jpn. 1984 Feb;19(1):53-8.

    [3]. González-Puga C, et al. Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: synergism with pharmacological levels of melatonin. J Pineal Res. 2005 Oct;39(3):243-50.

    [4]. Bunney BS, et al. Further studies on the specificity of proglumide as a selective cholecystokinin antagonist in the central nervous system. Ann N Y Acad Sci. 1985;448:345-51.

    [5]. Tariq M, et al. Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats. J Pharmacol Exp Ther. 1987 May;241(2):602-7.

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