Proglumide sodium salt|99247-33-3|(丙谷胺钠；蒙胃顿钠)-陌孚医药/Medlife

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

目录号: PC10840 纯度: ≥98%

CAS No. :99247-33-3

商品编号	规格	价格	会员价	是否有货	数量
PC10840-100mg	100mg	¥764.00	请登录
PC10840-10mM (in 1mL DMSO)	10mM(in1mLDMSO)	¥840.00	请登录

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中文名称	Proglumide sodium salt
中文别名	丙谷胺;4-苯酰胺-5-二丙氨基-5-氧戊酸钠盐
英文名称	Proglumide sodium salt
英文别名	Pentanoic acid,4-(benzoylamino)-5-(dipropylamino)-5-oxo-, sodium salt (1:1);PROGLUMIDE SODIUM SALT;4-Benzoylamino-5-dipropylamino-5-oxopentanoic acid sodium-potassium salt;N-Benzoyl-N′,N′-dipropyl-DL-isoglutamine sodium-potassium salt
Cas No.	99247-33-3
分子式	C₁₈H₂₅N₂O₄Na
分子量	356.39
包装储存	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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.

性状

Solid

IC50 & Target[1][2]

Cholecystokinin (CCK)-A/B receptors

体外研究(In Vitro)

In an 体外研究 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.
The incubation of HT29 cells with Proglumide significantly reduces the [H]-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%.

Medlife 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.

Medlife 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)
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, stored under nitrogen

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

ClinicalTrial

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. [Information]

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

[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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (280.59 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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