化合物SLV319 T4654

Product Introduction
Bioactivity


英文名: (±)-Ibipinabant

描述: (±)-Ibipinabant ((±)-SLV319) 是一种有效选择性的大麻素-1 (CB-1) 受体拮抗剂，IC50=22 nM。(±)-SLV319 是 SLV319的消旋体。

动物实验: Rats: SLV319, rimonabant and rosiglitazone are suspended in a 10% dimethylacetamide, 10% cremophor, 10% ethanol and 70% water vehicle. Drugs are administered by oral gavage in a volume of 2 mL/kg body weight at 09:00 hours every day. Treatment groups are as follows: (i) Vehicle: ad libitum access to food (vehicle), (ii) Vehicle: restricted access to food (20% less than average food intake of ad libitum vehicle-treated group for the first 3 days of the study, then 10% less than the average food intake of the ad libitum vehicle-treated group for the remainder of the study) (restricted), (iii) Rosiglitazone (4 mg/kg), (iv) Rimonabant (3 mg/kg) (RIM 3 mg/kg), (v) Rimonabant (10 mg/kg) (RIM 10 mg/kg), (vi) SLV319 (3 mg/kg) (IBI 3 mg/kg) and (vii) Ibipinabant (10 mg/kg) (IBI 10 mg/kg). Rosiglitazone is used as a positive control for its ability to delay β-cell decline, and rimonabant is used as a positive control for CB1 antagonism[3].

体外活性: 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 [Ki (CB1)=7.8 nM] and selective [Ki (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].

体内活性: Ibipinabant (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 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (92.33 mM)


关键字: SLV 319 | Inhibitor | (±)-Ibipinabant | BMS6462 | SLV-319 | Cannabinoid Receptor | BMS 6462 | (±) Ibipinabant | BMS-6462 | Ibipinabant | inhibit | (±)Ibipinabant

相关产品: CB 65 | CB1-IN-1 | CB1R/AMPK modulator 1 | CB2R agonist 2 | Tetrahydromagnolol | 6-Iodopravadoline | 2'-Hydroxydaidzein | JHU 75528 | Rimonabant hydrochloride | CB1 antagonist 1

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | GPCR Compound Library | Anti-Obesity Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library

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