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Loxiglumide

Cat. No. M8234
Loxiglumide Structure
Synonym:

CR-1505

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Biological Activity

Loxiglumide is a small-molecule antagonist of the cholecystokinin receptor CCKA. Loxiglumide inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying.

Chemical Information
Molecular Weight 461.38
Formula C21H30Cl2N2O5
CAS Number 107097-80-3
Solubility (25°C) DMSO: ≥5 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] Martin Katschinski. Loxiglumide Rotta research

[2] K Satake, et al. Therapeutic effects of loxiglumide on experimental acute pancreatitis using various models

[3] M Otsuki, et al. Treatment with cholecystokinin receptor antagonist loxiglumide enhances insulin response to intravenous glucose stimulation in postpancreatitic rats

[4] C Niederau, et al. Effects of loxiglumide on gallbladder emptying in healthy volunteers

[5] W E Schmidt, et al. Role of CCK in regulation of pancreaticobiliary functions and GI motility in humans: effects of loxiglumide

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