Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ibipinabant (SLV319) is a potent, selective, and orally active antagonist of the cannabinoid CB1 receptor, demonstrating a K i of 7.8 nM and exhibiting over 1000-fold selectivity for CB1 compared to CB2 (K i =7943 nM). It is utilized in obesity and diabetes research [1] [2] [3].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 35 days | $ 198.00 | |
5 mg | 35 days | $ 793.00 | |
10 mg | 35 days | $ 1,180.00 |
Description | Ibipinabant (SLV319) is a potent, selective, and orally active antagonist of the cannabinoid CB1 receptor, demonstrating a K i of 7.8 nM and exhibiting over 1000-fold selectivity for CB1 compared to CB2 (K i =7943 nM). It is utilized in obesity and diabetes research [1] [2] [3]. |
In vitro | SLV319 competitively inhibits CP-55940 (CB agonist) binding to the human CB1 receptor in CHO cells genetically modified to express this receptor, exhibiting an inhibition constant (K i) of 7.8 nM [1]. Furthermore, SLV319 dose-dependently antagonizes the WIN-55212 (CB1 agonist)-induced release of arachidonic acid in these cells, demonstrating a potency (pA2) of 9.9 [1]. |
In vivo | SLV319, administered orally at a dosage of 3 mg/kg/day for 28 days, effectively reduces food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obesity (DIO) mice, as well as reverses high-fat diet (HFD)-induced increases in adipose tissue leptin mRNA. At doses ranging from 3-10 mg/kg given daily via oral gavage for 56 days, SLV319 also demonstrates weight loss-independent antidiabetic effects and mitigates β-cell loss in a rat model of progressive β-cell dysfunction. Furthermore, SLV319 counters CB agonist (CP55940)-induced hypotension in rats and hypothermia in mice, showcasing ED 50 values of 5.5 and 3 mg/kg, respectively. In an animal model involving six-week-old male C57Bl/6J mice fed a diet of 60% calories from fat, resulting in body weights exceeding 42 g within 12-14 weeks, a similar dosage and administration method led to significant reductions in food intake, body weight, and adiposity in DIO mice. |
Molecular Weight | 487.4 |
Formula | C23H20Cl2N4O2S |
CAS No. | 464213-10-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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