SLV319

SKU: orb1222322

Description

SLV319 has been used in trials studying the treatment of Obesity and Obesity and Type 2 Diabetes.(In Vitro):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.(In Vivo):(±)-Ibipinabant ((±)-SLV319) (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 ((±)-SLV319) 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.

Key Properties

• CAS Number: 362519-49-1
• MW: 487.4
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₀Cl₂N₄O₂S
• SMILES: O=S(=O)(N=C(NC)N1CC(C(=N1)c2ccc(Cl)cc2)c3ccccc3)c4ccc(Cl)cc4
• Target: CB1
• Solubility: DMSO : ≥ 31 mg/mL; 63.60 mM

Bioactivity

• In Vivo:
  (±)-Ibipinabant ((±)-SLV319) (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 ((±)-SLV319) 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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

(±)-SLV319 | (±)-BMS6462

Quick Database Links

Gene Symbol

CB1