Ibipinabant  (Synonyms: SLV319; BMS-646256)

Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a K_i of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (K_i=7943 nM). Ibipinabant can be used for the research of obesity and diabetic^[1][2][3].

SLV319 displaces the specific CP-55940 (CB agonist) binding in CHO cells stably transfected with human CB1 receptor, with a K_i of 7.8 nM^[1].
SLV319 concentration dependently antagonizes WIN-55212 (CB1 agonist)-induced arachidonic acid release in CHO cells, with a pA2 of 9.9^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SLV319 (3 mg/kg/day; p.o. for 28 d) reduces the food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obesity (DIO) mice^[2].
SLV319 (3 mg/kg/day, p.o. for 28 d) reverses the HFD-induced increase in adipose tissue leptin mRNA^[2].
SLV319 (3-10 mg/kg; daily oral gavage for 56 d) has weight loss-independent antidiabetic effects and attenuates β-cell loss in a rat model of progressive β-cell dysfunction^[3].
SLV319 (oral administration) antagonizes CB agonist (CP55940) induced hypotension in rats and hypothermia in mice, with an ED₅₀ of 5.5 and 3 mg/kg, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

487.40

C₂₃H₂₀Cl₂N₄O₂S

464213-10-3

Solid

White to off-white

C/N=C(N1N=C(C2=CC=C(Cl)C=C2)[C@@H](C3=CC=CC=C3)C1)\NS(=O)(C4=CC=C(Cl)C=C4)=O

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Lange JHM, et, al. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. J Med Chem. 2004 Jan 29;47(3):627-43.  [Content Brief]

  [2]. Tam J, et, al. Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance. Cell Metab. 2012 Aug 8;16(2):167-79.  [Content Brief]

  [3]. Rohrbach K, et, al. Ibipinabant attenuates β-cell loss in male Zucker diabetic fatty rats independently of its effects on body weight. Diabetes Obes Metab. 2012 Jun;14(6):555-64.  [Content Brief]