Guvacine HCl

Cat No.:V4961 Purity: ≥98%

COA Product Data Instructions for use SDS

Guvacine HCl, the hydrochloride salt of Guvacine, is an alkaloid isolated from the nut ofAreca catechu whichacts 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).

Guvacine HCl Chemical Structure CAS No.: 6027-91-4
Product category: GABA Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators

Product Description

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).

Biological Activity I Assay Protocols (From Reference)

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].
References	[1]. 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]. 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]. 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.

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].

References

[1]. 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]. 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]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C6H10CLNO2
Molecular Weight	163.6021
Exact Mass	163.04
CAS #	6027-91-4
Related CAS #	Guvacine;498-96-4;Guvacine hydrobromide;6027-92-5
PubChem CID	11957555
Appearance	White to off-white solid powder
LogP	1.121
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	1
Heavy Atom Count	10
Complexity	151
Defined Atom Stereocenter Count	0
InChi Key	FGNUNVVTHHKDAM-UHFFFAOYSA-N
InChi Code	InChI=1S/C6H9NO2.ClH/c8-6(9)5-2-1-3-7-4-5;/h2,7H,1,3-4H2,(H,8,9);1H
Chemical Name	1,2,3,6-tetrahydropyridine-5-carboxylic acid;hydrochloride
HS Tariff Code	2934.99.9001
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)

Solubility Data

Solubility (In Vitro)	H2O : ~41.67 mg/mL (~254.71 mM) DMSO : ~1 mg/mL (~6.11 mM)
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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
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Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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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.

Note： (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.