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Vabicaserin hydrochloride

Catalog No. T13275 CAS 887258-94-8

Synonyms: SCA 136

Vabicaserin hydrochloride (SCA 136) is a selective agonist of 5-hydroxytryptamine 2C (5-HT2C) receptor (EC50: 8 nM).

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Vabicaserin hydrochloride Chemical Structure

Vabicaserin hydrochloride, CAS 887258-94-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 148.00
5 mg	In stock	$ 372.00
10 mg	In stock	$ 556.00
25 mg	In stock	$ 896.00
50 mg	In stock	$ 1,220.00
100 mg	In stock	$ 1,650.00
500 mg	In stock	$ 3,290.00
1 mL * 10 mM (in DMSO)	In stock	$ 397.00

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Purity: 98.42%

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Description	Vabicaserin hydrochloride (SCA 136) is a selective agonist of 5-hydroxytryptamine 2C (5-HT2C) receptor (EC50: 8 nM).
Targets&IC50	5-HT2C:8 nM (EC50)
In vitro	In Chinese hamster ovary cell membranes, Vabicaserin displaces 125I-(2,5-dimethoxy)phenylisopropylamine binding from human 5-HT2C receptor sites (Ki: 3 nM) and is >50-fold selective over a number of serotonergic, noradrenergic, and dopaminergic receptors. The binding affinity determined for the human 5-HT2B receptor subtype using [3H]5HT is 14 nM. Vabicaserin is a potent and full agonist (EC50, 8 nM; Emax, 100%) in stimulating 5-HT2C receptor-coupled calcium mobilization and exhibits 5-HT2A receptor antagonism and 5-HT2B antagonist or partial agonist activity in transfected cells, depending on the level of receptor expression. Vabicaserin showed a lower affinity at the binding site (22 nM) of 5-HT2C antagonist labeled with [3H]methsulamide. Other binding studies have shown that Vabicaserin has an affinity for 5-HT2B and 5-HT1A receptors with Ki values of 14 and 112 nM, respectively [1].
In vivo	After administering a single oral dose of [14C]Vabicaserin (50 mg/kg in mice, 5 mg/kg in rats, and 15 mg/kg in dogs), the unchanged drug accounted for less than 19%, 20%, and 35% of the total plasma radioactivity in mice, rats, and dogs, respectively, at all examined time points. The carbamoyl glucuronide (CG) comprised approximately 7-36% of plasma radioactivity in mice, 2-28% in dogs, and was absent in rat plasma following the single [14C]Vabicaserin dose, yet observed in rat plasma after multiple-dose administration of Vabicaserin at higher doses, being roughly 20 times lower than Vabicaserin based on AUC0-24 values at steady state. The plasma AUC0-24 ratios of CG to Vabicaserin were 1.5 in mice and 1.7 in dogs post-single dose. At doses used for safety assessment, these ratios at steady state were lower for mice (0.2-0.6) but slightly higher for dogs (1.8-4.0). CG was detected in dog urine at amounts comparable to the parent drug but was not found in mouse or rat urine post-single dose. Following a 5 mg/kg [14C]Vabicaserin dose in rats, 19-24% of the administered dose was recovered in bile over 24 hours, with CG representing up to 30% of biliary radioactivity. In monkeys, after a single oral 25-mg/kg dose of Vabicaserin, CG plasma concentrations surpassed those of Vabicaserin at all examined postdose intervals (2-24 h), though the CG-to-Vabicaserin ratio declined by 24 h postdose, from 17.5 at 2 h to 1.7 at 24 h, indicating that CG is a major metabolite with a 12:1 AUC0-24 ratio to Vabicaserin.

Synonyms	SCA 136
Molecular Weight	264.79
Formula	C15H21ClN2
CAS No.	887258-94-8

Storage

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

Solubility Information

DMSO: 75 mg/mL (283.24 mM), Sonication is recommended.

H2O: 4 mg/mL (15.11 mM), Sonication is recommended.

References and Literature

1. 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. 2. Tong Z, et al. Species differences in the formation of Vabicaserin carbamoyl glucuronide. Drug Metab Dispos. 2010 Apr;38(4):581-90.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Neurotransmitter Receptor Compound Library Bioactive Compound Library Antidepressant Compound Library Neuronal Signaling Compound Library

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Keywords

Vabicaserin hydrochloride 887258-94-8 GPCR/G Protein Neuroscience 5-HT Receptor SCA136 inhibit 5-hydroxytryptamine Receptor Vabicaserin Inhibitor SCA 136 Vabicaserin Hydrochloride Serotonin Receptor SCA-136 inhibitor

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