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Proglumide

Cat. No. M10420
Proglumide Structure
Size Price Availability Quantity
50mg USD 58  USD58 In stock
100mg USD 100  USD100 In stock
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Quality Control & Documentation
Biological Activity

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. 

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.

Chemical Information
Molecular Weight 334.41
Formula C18H26N2O4
CAS Number 6620-60-6
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

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

[2] Y Iwamoto, et al. Gastroenterol Jpn. In vitro and in vivo effect of proglumide on cholecystokinin-stimulated amylase release in mouse pancreatic acini

[3] M Tariq, et al. J Pharmacol Exp Ther. Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats

[4] B S Bunney, et al. Ann N Y Acad Sci. Further studies on the specificity of proglumide as a selective cholecystokinin antagonist in the central nervous system

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