Ibipinabant (SLV319) 是一种有效，选择性和具有口服活性的大麻素 CB1 受体 (cannabinoid CB1 receptor) 的拮抗剂，Ki值为 7.8 nM。Ibipinabant 对 CB1 的选择性比对 CB2 (Ki=7943 nM) 的选择性高 1000 倍以上。Ibipinabant 可用于肥胖和糖尿病的研究。
| 生物活性 | Ibipinabant (SLV319) is a potent, selective and orally active antagonist ofcannabinoidCB1receptor, with aKiof 7.8 nM. Ibipinabant shows more than 1000-fold selectivity forCB1overCB2(Ki=7943 nM). Ibipinabant can be used for the research of obesity and diabetic[1][2][3]. |
| IC50& Target[1] | CB1 7.8 nM (Ki) | CB2 7943 nM (Ki) |
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体外研究
(In Vitro) | SLV319 displaces the specific CP-55940 (CB agonist) binding in CHO cells stably transfected with human CB1 receptor, with a Kiof 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].
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体内研究
(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 ED50of 5.5 and 3 mg/kg, respectively[1].
| Animal Model: | Six-week-old male C57Bl/6J mice received a diet containing 60% of calories as fat, resulting in body weights >42 g in 12-14 weeks[2] | | Dosage: | 3 mg/kg/day | | Administration: | P.o. for 28 days | | Result: | Caused reductions in food intake, body weight and adiposity in DIO mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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