Proglumide
目录号: PL05499 纯度: ≥99%
CAS No. :6620-60-6
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中文名称
Proglumide
中文别名
丙谷胺;二丙谷酰胺;()-5-二丙基氨基-4-苯甲酰氨基-5-氧代-戊酸;8-氨基异喹啉-1-醇;丙谷酰胺;(+/-)-5-二丙基氨基-4-苯甲酰氨 基-5-氧代戊酸 ,丙;(+/-)-5-二丙基氨基-4-苯甲酰氨基-5-氧代戊酸;(±)-5-二丙基氨基-4-苯甲酰氨基-5-氧代-戊酸
英文名称
Proglumide
英文别名
4-Benzamido-5-(dipropylamino)-5-oxopentanoic acid;4-benzamido-N,N-dipropyl-DL-glutaramic acid;Proglumide;Binoside;Gastrotopic;Midelid;Milide;N-Benzoyl-N',N'-dipropyl-DL-isoglutamine;N-benzoyl-N',N'-dipropyl-RS-isoglutamine;Nulsa;Ulcutin;Xyde;Xylamide;(+/-)-4-Benzamido-N,N-dipropylglutaramic acid
Cas No.
6620-60-6
分子式
C18H26N2O4
分子量
334.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Proglumide 是一种非肽和口服活性胆囊收缩素 (CCK)-A/B 受体拮抗剂。Proglumide 选择性阻断 CCK 在中枢神经系统中的作用。Proglumide 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 is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide 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 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.
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%. has not independently confirmed the accuracy of these methods.
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
[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.
溶解度数据
In Vitro: DMSO : ≥ 65 mg/mL (194.37 mM)配制储备液
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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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