在体外研究中，浓度为 0.3 至 10 mM 的丙谷胺可减少 CCK 刺激的淀粉酶释放；浓度在 0 至 3 mM 之间时，丙谷胺对基线淀粉酶释放没有影响。随着丙谷胺浓度的升高，淀粉酶产生的CCK的剂量反应曲线向右移动。丙谷胺的抑制作用是可逆的。 Proglumide 对 CCK 和相关肽也具有选择性影响 [2]。丙谷胺处理 HT29 细胞时，IC50 为 6.5 mM，以剂量依赖性方式显着减少 [3H]-胸苷掺入 HT29 细胞中。 Proglumide 可使细胞凋亡增加高达 70%，同时以剂量依赖性方式降低坏死百分比 [3]。

Proglumide（250-750 mg/kg；腹腔注射；成年雄性 Sprague-Dawley 大鼠）是一种有效的治疗方法，可大大减少大脑氧化应激、认知障碍和癫痫发作活动 [1]。

Animal/Disease Models: Induction of status epilepticus (SE) in adult male Sprague Dawley rats (200-250 g; 2 months old) [1]
Doses: 250 mg/kg, 500 mg/kg, and 750 mg/kg
Route of Administration: Results of intraperitoneal (ip) injection: dose-dependent and significant increase in seizure and SE latency. Significant and dose-dependent attenuated Li-PC (SE)-induced increases in thiobarbituric acid (TBARS) and catalase (CAT), attenuated Li-Pc-induced decreases in SOD, and attenuated GSH and Depletion of glutathione-S transferase (GST). Hippocampus and striatum.

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

Proglumide is a racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for treatment of stomach ulcers, but has been replaced by newer drugs. It has a role as a drug metabolite, a xenobiotic metabolite, a cholinergic antagonist, an anti-ulcer drug, a cholecystokinin antagonist, a gastrointestinal drug, a delta-opioid receptor agonist and an opioid analgesic. It contains a (R)-proglumide and a (S)-proglumide.
Proglumide is an orally bioavailable cholecystokinin (CCK) receptor antagonist, with gastric acid reducing and potential antineoplastic activities. Upon oral administration, proglumide binds to and blocks both cholecystokinin receptor type A (CCK-AR; CCK1-R) and gastrin/cholecystokinin type B receptor (CCK-BR; CCK2-R). This prevents the binding of cholecystokinin and gastrin to the CCK receptors, and inhibits both gastrointestinal (GI) motility and gastric secretions. This may also decrease fibrosis in the tumor microenvironment (TME), increase both the infiltration of T-cells and the penetration of chemotherapeutic agents, and inhibit tumor growth and metastasis. CCK receptors, normally expressed in the GI tract and the nervous system, are overexpressed on fibroblasts and certain cancers.
A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

334.189

6620-60-6

Proglumide sodium;99247-33-3;Proglumide hemicalcium;85068-56-0

4922

White to off-white solid powder

1.1±0.1 g/cm3

589.8±45.0 °C at 760 mmHg

148.5--152ºC

310.5±28.7 °C

0.0±1.7 mmHg at 25°C

1.534

2.53

86.71

2

4

10

24

413

0

O=C(O)CCC(NC(C1=CC=CC=C1)=O)C(N(CCC)CCC)=O

DGMKFQYCZXERLX-UHFFFAOYSA-N

InChI=1S/C18H26N2O4/c1-3-12-20(13-4-2)18(24)15(10-11-16(21)22)19-17(23)14-8-6-5-7-9-14/h5-9,15H,3-4,10-13H2,1-2H3,(H,19,23)(H,21,22)

4-benzamido-5-(dipropylamino)-5-oxopentanoic acid

Proglumide W-5219 W 5219W5219

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 65 mg/mL (~194.37 mM)

配方 1 中的溶解度: ≥ 2.17 mg/mL (6.49 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 21.7 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.17 mg/mL (6.49 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 21.7 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.17 mg/mL (6.49 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 21.7 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。