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Bevenopran

Cat. No. M21657
Bevenopran Structure
Synonym:

CB-5945; ADL-5945

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Biological Activity

Bevenopran (CB-5945) is a peripheral μ-opioid receptor antagonist. Bevenopran tends to increase bowel movement (BM) frequency, especially for 0.1 mg twice daily and 4 mg daily, respectively.

Chemical Information
Molecular Weight 386.44
Formula C20H26N4O4
CAS Number 676500-67-7
Solubility (25°C) DMSO ≥ 90 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] Jasper Pannemans, et al. United European Gastroenterol J. New developments in the treatment of opioid-induced gastrointestinal symptoms

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Keywords: Bevenopran, CB-5945; ADL-5945 supplier, Opioid Receptor, inhibitors, activators


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