Guvacine hydrochloride
Based on 1 publication(s) in Google Scholar
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 6027-91-4
- Formula: C6H10ClNO2
- Molecular Weight:163.60
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Storage:
-20°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
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Guvacine hydrochloride
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Biological Activity
IC50: 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), 1870 μM (human BGT-3)[1]
Guvacine hydrochloride is a potent inhibitor of GABA transporter, dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3). Guvacine has low affinity at hBGT-1 (IC50 >1 mM)[1]. Guvacine hydrochloride is a potent inhibitor of GABA uptake, but does not inhibit sodium-independent GABA binding, and is weak or inactive as a GABA receptor agonist[2]. Guvacine inhibits the uptake GABA and β-alanine with IC50s of 23 ± 2 μM, 66 ± 11 μM in the Cat spinal cord, and 8 ± 1 μM, 123 ± 28 μM in the rat cerebral cortex, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 6027-91-4
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Appearance Solid
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Molecular Weight 163.60
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Formula C6H10ClNO2
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Color White to off-white
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SMILES
O=C(C1=CCCNC1)O.[H]Cl
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Commun Biol
RBAP48 facilitates the oral squamous cell carcinoma process in an androgen receptor-dependent and independent manners. [Abstract]2025 May 30;8(1):829. PMID: 40442479
Solvent & Solubility
H2O : 41.67 mg/mL (254.71 mM; Need ultrasonic)
DMSO : 10 mg/mL (61.12 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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)
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: 25 mg/mL (152.81 mM); Clear solution; Need ultrasonic
Protocol
Cells grown in 24-well plates are washed 3 × with Hepes-buffered saline (HBS, in mM: NaC1, 150; Hepes, 20; CaCl2, 1; glucose, 10; KC1, 5; MgCl2, 1; pH 7.4) and allowed to equilibrate on a 37°C slide warmer. After 10 min the medium is removed and unlabeled drugs (Guvacine , etc.) in HBS are added (450 μL/well). Transport is initiated by adding 50 μL per well of a concentrated solution of [3H]GABA in HBS (final concentration = 50 nM). Non-specific uptake is defined in parallel wells with 1 mM unlabeled GABA, and is subtracted from total uptake to yield specific uptake; all data represent specific uptake. Plates are incubated at 37°C for 10 min, then washed rapidly 3 × with ice-cold HBS, using a 24-position plate washer. Cells are solubilized with 0.05% sodium deoxycholate/0.1 N NaOH (0.25 mL/well), an aliquot neutralized with 1 N HC1, and radioactivity is determined by scintillation counting. Protein is quantified in an aliquot of the solubilized cells using a BIO-RAD protein assay kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Borden LA, et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24. [Content Brief]
[2]. Krogsgaard-Larsen P, et al. Structure-activity studies on the inhibition of GABA binding to rat brain membranes by muscimol and related compounds. J Neurochem. 1978 Jun;30(6):1377-82. [Content Brief]
[3]. Lodge D, et al. Effects of the Areca nut constituents arecaidine and guvacine on the action of GABA in the cat central nervous system. Brain Res. 1977 Nov 18;136(3):513-22. [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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 6.1125 mL | 30.5623 mL | 61.1247 mL | 152.8117 mL |
| 5 mM | 1.2225 mL | 6.1125 mL | 12.2249 mL | 30.5623 mL | |
| 10 mM | 0.6112 mL | 3.0562 mL | 6.1125 mL | 15.2812 mL | |
| 15 mM | 0.4075 mL | 2.0375 mL | 4.0750 mL | 10.1874 mL | |
| 20 mM | 0.3056 mL | 1.5281 mL | 3.0562 mL | 7.6406 mL | |
| 25 mM | 0.2445 mL | 1.2225 mL | 2.4450 mL | 6.1125 mL | |
| 30 mM | 0.2037 mL | 1.0187 mL | 2.0375 mL | 5.0937 mL | |
| 40 mM | 0.1528 mL | 0.7641 mL | 1.5281 mL | 3.8203 mL | |
| 50 mM | 0.1222 mL | 0.6112 mL | 1.2225 mL | 3.0562 mL | |
| 60 mM | 0.1019 mL | 0.5094 mL | 1.0187 mL | 2.5469 mL | |
| H2O | 80 mM | 0.0764 mL | 0.3820 mL | 0.7641 mL | 1.9101 mL |
| 100 mM | 0.0611 mL | 0.3056 mL | 0.6112 mL | 1.5281 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.
Guvacine hydrochloride Related Classifications
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