Vabicaserin hydrochloride NEW
| Price | $76 | $188 | $278 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Vabicaserin hydrochloride | CAS No.: 887258-94-8 |
| Purity: 98.42% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Vabicaserin hydrochloride |
| Description | Vabicaserin hydrochloride (SCA 136) is a selective agonist of 5-hydroxytryptamine 2C (5-HT2C) receptor (EC50: 8 nM). |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (207.71 mM), Sonication is recommended. H2O : 4 mg/mL (15.11 mM), Sonication is recommended. |
| Keywords | Vabicaserin Hydrochloride | Vabicaserin hydrochloride | Vabicaserin | Serotonin Receptor | SCA-136 | SCA136 | Inhibitor | inhibit | 5-hydroxytryptamine Receptor | 5-HT Receptor |
| Inhibitors Related | Serotonin hydrochloride | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Mirtazapine | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Neurotransmitter Receptor Compound Library | Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Serotonin Receptor-Targeted Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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- Address: 36?Washington?Street, Wellesley?Hills
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