Vabicaserin hydrochloride
Based on 5 publication(s) in Google Scholar
Vabicaserin hydrochloride (SCA-136) is a brain-penetrant, orally active, and selective 5-HT2C receptor agonist (Ki = 3 nM; EC50 = 8 nM). Vabicaserin hydrochloride specifically activates Gq-coupled 5-HT2C receptors to promote calcium mobilization, thereby selectively reducing dopamine release in the mesolimbic system without affecting the nigrostriatal pathway. Vabicaserin hydrochloride is an antagonist of 5-HT2A/5-HT2B receptors. Vabicaserin hydrochloride can be used for research on schizophrenia, obesity, chronic pain, and neurodegenerative diseases (such as Machado-Joseph disease).
For research use only. We do not sell to patients.
- Purity : 99.47%
- CAS No.: 887258-94-8
- Formula: C15H21ClN2
- Molecular Weight:264.79
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Vabicaserin hydrochloride
MoreAll 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[6]|
Human 5-HT2C Receptor 3 nM (Ki) |
human 5-HT2B Receptor 14 nM (Ki) |
human 5-HT1A Receptor 112 nM (Ki) |
5-HT2C Receptor 8 nM (EC50) |
5-HT2A Receptor 1650 nM (EC50) |
5-HT2B Receptor 29 nM (EC50) |
In Vitro
Vabicaserin (SCA-136 free base) binds to the human 5-HT2C receptor with high affinity (Ki = 3 nM) and exhibits greater than 50-fold selectivity over other monoamine receptors, with affinity for the 5-HT2B (Ki = 14 nM) and 5-HT1A (Ki = 112 nM) receptors[6].
Vabicaserin is a potent and full 5-HT2C receptor agonist (EC50 = 8 nM) in CHO cells and acts as an antagonist at 5-HT2A (IC50 = 1650 nM) and 5-HT2B (IC50 = 29 nM) receptors, with its 5-HT2B agonist activity depending on receptor expression levels[6].
Vabicaserin (30 min) promotes the accumulation of 5-HT2C-coupled inositol monophosphate (IP1) in CHO cells with an EC50 of 32 nM[6].
Vabicaserin exhibits activity in increasing the frequency of spontaneous or NKA (HY-P0197)-induced rhythmic contractions in human distal ureteral tissue cell strips[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Vabicaserin ameliorates mutant ATXN3-mediated motor dysfunction in the C. elegans AT3q130 model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rat (male; 250-300g) subcutaneously injected of 1 mg/kg Reserpine once daily for 3 consecutive days[8]
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Dosage:0.3, 1, 3 mg/kg
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Administration:s.c.; single dose; 30, 60, 120, 240 min
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Result:Recovered the muscle pressure threshold at doses of 1 and 3 mg/kg.
Alleviated myalgia without producing a significant reduction in locomotor activity.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 887258-94-8
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Appearance Solid
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Molecular Weight 264.79
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Formula C15H21ClN2
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Color Light yellow to yellow
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SMILES
[H][C@]1(CCC2)[C@]2([H])CN3C(C1=CC=C4)=C4CNCC3.Cl
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Synonyms
SCA-136
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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ACS Chem Neurosci
2025 Oct 1;16(19):3899-3914. PMID: 40944639 -
Neuroscience
Selective Serotonin Reuptake Inhibitors and 5-HT2 Receptor Agonists Have Distinct, Sleep-state Dependent Effects on Postictal Breathing in Amygdala Kindled Mice. [Abstract]2023 Mar 1:513:76-95. PMID: 36702372 -
Epilepsy Behav
MK-212 precipitates seizure-induced death in amygdala-kindled mice via a non-5-HT2C receptor-mediated mechanism. [Abstract]2025 Jun:167:110385. PMID: 40132446 -
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Solvent & Solubility
In Vitro:
DMSO : 60 mg/mL (226.59 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4 mg/mL (15.11 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 5 mg/mL (18.88 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
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Data Sheet (295 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Chen W. Repeated administration of 5‐hydroxytryptamine 2C agonist MK212 produces a sensitization effect of antipsychotic activity. IUBMB life. 2016 Dec;68(12):985-93. [Content Brief]
[6]. Dunlop J, et al. Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist. The Journal of pharmacology and experimental therapeutics. 2011 Jun;337(3):673-80. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.7766 mL | 18.8829 mL | 37.7658 mL | 94.4144 mL |
| 5 mM | 0.7553 mL | 3.7766 mL | 7.5532 mL | 18.8829 mL | |
| 10 mM | 0.3777 mL | 1.8883 mL | 3.7766 mL | 9.4414 mL | |
| 15 mM | 0.2518 mL | 1.2589 mL | 2.5177 mL | 6.2943 mL | |
| DMSO | 20 mM | 0.1888 mL | 0.9441 mL | 1.8883 mL | 4.7207 mL |
| 25 mM | 0.1511 mL | 0.7553 mL | 1.5106 mL | 3.7766 mL | |
| 30 mM | 0.1259 mL | 0.6294 mL | 1.2589 mL | 3.1471 mL | |
| 40 mM | 0.0944 mL | 0.4721 mL | 0.9441 mL | 2.3604 mL | |
| 50 mM | 0.0755 mL | 0.3777 mL | 0.7553 mL | 1.8883 mL | |
| 60 mM | 0.0629 mL | 0.3147 mL | 0.6294 mL | 1.5736 mL | |
| 80 mM | 0.0472 mL | 0.2360 mL | 0.4721 mL | 1.1802 mL | |
| 100 mM | 0.0378 mL | 0.1888 mL | 0.3777 mL | 0.9441 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Vabicaserin hydrochloride Related Classifications
HY-111200 Related Classifications
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