Vabicaserin hydrochloride, Inhibitor

Vabicaserin hydrochloride

Cat. Num. AAA5754089

• Purity: 98.00%
• Synonyms: Vabicaserin hydrochloride; SCA 136; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 75mg/mL (283.24mM) Need ultrasonic; H2O: 4mg/mL (15.11mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C15H21ClN2
• SMILES: [H][C@@]12C3=CC=CC4=C3N(CCNC4)C[C@]1([H])CCC2.Cl
• CAS Number: 887258-94-8
• Target & IC50: 5-HT2C Receptor: ic50 8nM (EC50)
• In Vitro: Unchanged drug represents less than 19, 20, and 35% of total plasma radioactivity at all the time points examined in mice, rats, and dogs, respectively,after a single oral dose of [14C]Vabicaserin at 50, 5, and 15mg/kg. The carbamoyl glucuronide (CG) represents approximately 7 to 36% of plasma radioactivity in mice and 2 to 28% of plasma radioactivity in dogs but is not detected in rat plasma after the single [14C]Vabicaserin dose. However, the CG is observed in rat plasma after multiple-dose administration of Vabicaserin at higher doses, and the CG is approximately 20 times less than Vabicaserin based on steady-state AUC0-24 values. The estimated plasma AUC0-24 ratios of CG to the parent drug are 1.5 and 1.7 in mice and dogs after the single [14C]Vabicaserin dose, respectively. The plasma AUC0-24 ratios for the CG to Vabicaserin at steady state with doses used for safety assessment are less for mice (0.2-0.6) and slightly higher for dogs (1.8-4.0) compared with the single dose values. The CG is detected in dog urine in similar amounts to the parent drug, although it is not detected in mouse or rat urine after the single [14C]Vabicaserin dose. Radioactivity in a 0- to 24-h bile collection from rats receiving a 5mg/kg [14C]Vabicaserin dose accounts for 19 and 24% of the administered dose in males and females, respectively. Although the CG is not detected in urine or feces of rats after a single oral administration, In male rats and 15% in female rats, it represents an average of up to 30% of biliary radioactivity. In monkeys after a single oral 25-mg/kg dose of Vabicaserin, the plasma concentrations of the CG exceeded those of Vabicaserin at all the time points (2-24 h) postdose, although the amount of CG relative to Vabicaserin decreased by 24 hours postdose, with ratios of 17.5 at 2 h and 1.7 at 24 hours. In monkeys, The CG to Vabicaserin AUC0-24 ratio of 12:1 indicates that the CG is a major metabolite [2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Vabicaserin hydrochloride, inhibitor

Vabicaserin hydrochloride is a selective agonist of 5-hydroxytryptamine 2C (5-HT2C) receptor (EC50: 8nM).

References

Dunlop J, et al. Characterization of Vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist. J Pharmacol Exp Ther. 2011 Jun;337(3):673-80.
Dunlop J, et al. Characterization of Vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist. J Pharmacol Exp Ther. 2011 Jun;337(3):673-80.
Tong Z, et al. Species differences in the formation of Vabicaserin carbamoyl glucuronide. Drug Metab Dispos. 2010 Apr;38(4):581-90.
Tong Z, et al. Species differences in the formation of Vabicaserin carbamoyl glucuronide. Drug Metab Dispos. 2010 Apr;38(4):581-90.