Proglumide sodium is a non-peptide and orally bioactive cholecystokinin (CCK)-A/B receptor blocker (antagonist). Proglumide sodium selectively blocks the effects of CCK in the central nervous system. Proglumide sodium has the ability to inhibit gastric secretion and protect the gastroduodenal mucosa, and also has antiepileptic and anti-oxidant effects.

Physicochemical Properties

Molecular Formula	C18H25N2O4NA
Molecular Weight	356.3919
Exact Mass	356.171
CAS #	99247-33-3
Related CAS #	Proglumide;6620-60-6;Proglumide hemicalcium;85068-56-0
PubChem CID	23677833
Appearance	White to off-white solid powder
LogP	1.538
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	10
Heavy Atom Count	25
Complexity	419
Defined Atom Stereocenter Count	0
InChi Key	UFMWGCINVOIJSO-UHFFFAOYSA-M
InChi Code	InChI=1S/C18H26N2O4.Na/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);/q;+1/p-1
Chemical Name	sodium;4-benzamido-5-(dipropylamino)-5-oxopentanoate
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Proglutamine at concentrations of 0.3–10 mM quantitatively suppressed CCK-stimulated amylase production in an in vitro investigation, but proglutamine at values of 0–3 mM had no effect on basal amylase. liberated. The dose-response curve of amylase release vs CCK moves to the right as proglutamine concentration rises. Proglumide's inhibitory action is reversible. Proglumide is additionally selective for CCK and related peptides [2]. Proglumide dosage dramatically decreased [3H]-bust daily injection into HT29 cells with an IC50 of 6.5 mM in a dose-dependent manner. Proglumide has a dose-dependent effect in reducing the overall number of questions, with a dose-dependence of up to 70% on cells [3].
ln Vivo	Proglumide treatment (250–750 mg/kg; intraperitoneal injection; adult Sprague Dawley Project) dramatically reduces brain oxidation, cognitive dysfunction, and engineering activity [1].
Animal Protocol	Animal/Disease Models: Adult male Sprague Dawley rats (200) -250 g; 2 months old) induced status epilepticus (SE) [1] Doses: 250 mg/kg, 500 mg/kg and 750 mg/kg administered Methods: intraperitoneal (ip) injection Experimental Results: Dose-dependent and significant increase in latency to seizures and SE. 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.
References	[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.

Solubility Data

Solubility (In Vitro)	H2O : ~100 mg/mL (~280.59 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 100 mg/mL (280.59 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.