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Ibipinabant

Cat. No. M30122
Ibipinabant Structure
Synonym:

SLV319; BMS-646256

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Quality Control & Documentation
Biological Activity

Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a Ki of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (Ki=7943 nM). Ibipinabant can be used for the research of obesity and diabetic.

Chemical Information
Molecular Weight 487.4
Formula C23H20Cl2N4O2S
CAS Number 464213-10-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Bhupender Nehra, et al. Eur J Med Chem. Recent advancements in the development of bioactive pyrazoline derivatives

[2] Tom J J Schirris, et al. Sci Rep. Mitochondrial ADP/ATP exchange inhibition: a novel off-target mechanism underlying ibipinabant-induced myotoxicity

[3] Michael M Leane, et al. Pharm Dev Technol. Formulation and process design for a solid dosage form containing a spray-dried amorphous dispersion of ibipinabant

[4] K Rohrbach, et al. Diabetes Obes Metab. Ibipinabant attenuates β-cell loss in male Zucker diabetic fatty rats independently of its effects on body weight

[5] Wayne Sinclair, et al. J Pharm Sci. Physical stability and recrystallization kinetics of amorphous ibipinabant drug product by fourier transform raman spectroscopy

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Keywords: Ibipinabant, SLV319; BMS-646256 supplier, Cannabinoid, inhibitors, activators


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