| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Guvacine HCl, the hydrochloride salt of Guvacine, is an alkaloid isolated from the nut of Areca catechu which 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).
| ln Vitro |
GuvacineHClide has IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), and 58 μM (rat GAT-2); 119 μM (human GAT-3); 378 μM (rat GAT-3) and 1870 μM (human BGT-3). It is a strong inhibitor of GABA transporters with moderate selectivity for cloned GABA transporters. Guvacine's affinity (IC50 > 1 mM) for hBGT-1 is low [1]. Guvacine hydrochloride is a strong inhibitor of GABA uptake, although it has little or no effect as a GABA receptor agonist and does not prevent sodium-dependent GABA binding [2]. Guvacine inhibits the absorption of GABA and β-alanine, with IC50s in the cat spinal cord of 23 ± 2 μM and 66 ± 11 μM, respectively, and in the rat cerebral cortex of 8 ± 1 μM and 123 ± 28 μM [3].
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| 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.
[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. [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 |
| Molecular Formula |
C6H10CLNO2
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|---|---|
| Molecular Weight |
163.6021
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| CAS # |
6027-91-4
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| Related CAS # |
Guvacine;498-96-4;Guvacine hydrobromide;6027-92-5
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| SMILES |
O=C(C1=CCCNC1)O.[H]Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~41.67 mg/mL (~254.71 mM)
DMSO : ~1 mg/mL (~6.11 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (152.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.1125 mL | 30.5623 mL | 61.1247 mL | |
| 5 mM | 1.2225 mL | 6.1125 mL | 12.2249 mL | |
| 10 mM | 0.6112 mL | 3.0562 mL | 6.1125 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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