| Bioactivity | 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[1][2][3]. |
| Invitro | SLV319 displaces the specific CP-55940 (CB agonist) binding in CHO cells stably transfected with human CB1 receptor, with a Ki 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]. |
| In Vivo | 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]. Animal Model: |
| Name | Ibipinabant |
| CAS | 464213-10-3 |
| Formula | C23H20Cl2N4O2S |
| Molar Mass | 487.40 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. [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. |
Ibipinabant
CAS: 464213-10-3 F: C23H20Cl2N4O2S W: 487.40
Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a Ki of 7.8 n
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