tcsc6430 (±) -Ibipinabant

(±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC₅₀ of 22 nM.

IC50 & Target: IC50: 22 nM (CB-1)^[1]; Ki: 7.8 nM (CB-1)^[2]

In Vitro: Cannabinoid receptor 1 (CB1R) antagonists appear to be promising drugs for the treatment of obesity, however, serious side effects have hampered their clinical application. Ibipinabant is a new, potent [K_i (CB1)=7.8 nM] and selective [K_i (CB2)=7.943 nM] CB1 antagonist [pA2 for arachidonic acid release in CHO cells=9.9] with in vitro pharmacological characteristics similar to rimonabant including inverse agonism and brain penetrance^[3].

In Vivo: (±)-Ibipinabant ((±)-SLV319) (3 mg/kg) reduces unfasted glucose to a significantly greater degree than rimonabant at the same dose on days 17, 28 and 38. Chronic treatment with (±)-Ibipinabant ((±)-SLV319) significantly attenuates the progression of diabetes in ZDF rats, blunting the increase in blood glucose and HbA1c over time. Ibipinabant also reduces the hyperinsulinemia apparent at 6-8 weeks of age and attenuates the dramatic reduction in insulin levels observed 1-2 weeks later^[3].