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Proglumide sodium salt

Cat. No. M7161
Proglumide sodium salt Structure
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Biological Activity

Proglumide sodium salt is a non-selective cholecystokinin (CCK) antagonist. Inhibits CCK-stimulated amylase secretion and prevents CCK-induced 2-deoxyglucose uptake in mouse pancreatic acini. Blocks growth of HT29 colon carcinoma cells in response to gastrin 17 treatment. Orally active.

Chemical Information
Molecular Weight 356.39
Formula C18H25N2NaO4
CAS Number 99247-33-3
Solubility (25°C) Water 35.64 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] Qiao, et al. Med Chem. Triphenylethanamine derivatives as cholesteryl ester transfer protein inhibitors: discovery of N-[(1R)-1-(3-cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamid J.

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