Ibipinabant - CAS 464213-10-3
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Cannabinoid Receptor
Ibipinabant is a potent and selective CB1 receptor antagonist with Ki values of 7.8 and 7,943 nM for CB1 and peripheral cannabinoid (CB2), respectively.
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White solid
(S)-SLV 319; BMS 646256; 3-(4-chlorophenyl)-N-[(4-chlorophenyl)sulfonyl]-4,5-dihydro-N'-methyl-4S-phenyl-1H-pyrazole-1-carboximidamide;
Soluble in DMSO
Store at -20 °C
Cannabinoid receptor CB1 antagonists
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
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1.Surface energy analysis as a tool to probe the surface energy characteristics of micronized materials--a comparison with inverse gas chromatography.
Gamble JF1, Leane M, Olusanmi D, Tobyn M, Supuk E, Khoo J, Naderi M. Int J Pharm. 2012 Jan 17;422(1-2):238-44. doi: 10.1016/j.ijpharm.2011.11.002. Epub 2011 Nov 10.
This study investigates the impact of micronization on the measured surface energy characteristics of an active pharmaceutical ingredient (API), ibipinabant, by inverse gas chromatography (IGC) using both a fixed probe concentration, commonly used in standard IGC methods, and a fixed probe surface coverage approach applied by the surface energy analyzer (SEA), a next generation IGC system. The IGC measurements indicate an initial increase in surface energy, going from un-micronized to micronized, followed by a reduction in surface energy with increasing micronization extent. This was attributable to the change in the retention behaviour of the dispersive probes as a consequence of the change in the probe surface coverage rather than a change in the actual surface energy of the materials being analysed. It was observed in the SEA data that micronization leads to an increase in the measured dispersive surface energy of the drug substance with increasing micronization extent.
2.Roller compaction: application of an in-gap ribbon porosity calculation for the optimization of downstream granule flow and compactability characteristics.
Gamble JF1, Tobyn M, Dennis AB, Shah T. Pharm Dev Technol. 2010 Jun;15(3):223-9. doi: 10.3109/10837450903095342.
This paper reports the use of an in-gap ribbon porosity calculation for the optimisation of roller compaction ribbon parameters in order to control downstream granule and tablet properties for a typical pharmaceutical formulation. The study demonstrates the effect of changes to roll speed and roll gap on the relative level of ribbon compaction for ribbons with equivalent in-gap porosities. It is demonstrated that in-gap ribbon porosity can be applied to enable optimization of the downstream granule processability characteristics for a typical pharmaceutical formulation and an understanding of the control space of a roller compaction process.
3.Cannabinoid receptor antagonist-induced striated muscle toxicity and ethylmalonic-adipic aciduria in beagle dogs.
Tomlinson L1, Tirmenstein MA, Janovitz EB, Aranibar N, Ott KH, Kozlosky JC, Patrone LM, Achanzar WE, Augustine KA, Brannen KC, Carlson KE, Charlap JH, Dubrow KM, Kang L, Rosini LT, Panzica-Kelly JM, Flint OP, Moulin FJ, Megill JR, Zhang H, Bennett MJ, Hor Toxicol Sci. 2012 Oct;129(2):268-79. doi: 10.1093/toxsci/kfs217. Epub 2012 Jul 21.
Ibipinabant (IBI), a potent cannabinoid-1 receptor (CB1R) antagonist, previously in development for the treatment of obesity, causes skeletal and cardiac myopathy in beagle dogs. This toxicity was characterized by increases in muscle-derived enzyme activity in serum and microscopic striated muscle degeneration and accumulation of lipid droplets in myofibers. Additional changes in serum chemistry included decreases in glucose and increases in non-esterified fatty acids and cholesterol, and metabolic acidosis, consistent with disturbances in lipid and carbohydrate metabolism. No evidence of CB1R expression was detected in dog striated muscle as assessed by polymerase chain reaction, immunohistochemistry, Western blot analysis, and competitive radioligand binding. Investigative studies utilized metabonomic technology and demonstrated changes in several intermediates and metabolites of fatty acid metabolism including plasma acylcarnitines and urinary ethylmalonate, methylsuccinate, adipate, suberate, hexanoylglycine, sarcosine, dimethylglycine, isovalerylglycine, and 2-hydroxyglutarate.
4.Ibipinabant attenuates β-cell loss in male Zucker diabetic fatty rats independently of its effects on body weight.
Rohrbach K1, Thomas MA, Glick S, Fung EN, Wang V, Watson L, Gregory P, Antel J, Pelleymounter MA. Diabetes Obes Metab. 2012 Jun;14(6):555-64. doi: 10.1111/j.1463-1326.2012.01563.x. Epub 2012 Feb 24.
AIM: To test the antidiabetic efficacy of ibipinabant, this new cannabinoid receptor 1 (CB1) antagonist was compared with food-restriction-induced weight loss, rosiglitazone (4 mg/kg) and rimonabant (3 and 10 mg/kg), using parameters of glycaemic control in male Zucker diabetic fatty (ZDF) rats.
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CAS 464213-10-3 Ibipinabant

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