Guvacine hydrochloride

Name: Guvacine hydrochloride
Brand: MedChemExpress
SKU: HY-100809
Rating: 4.5 (1 reviews)

製品番号: HY-100809 純度: 99.93%: Data Sheet SDS COA 取扱説明書
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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).

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Guvacine hydrochloride 構造式

CAS 番号 : 6027-91-4

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$50	在庫あり	Estimated Time of Arrival: December 31
10 mg	$70	在庫あり	Estimated Time of Arrival: December 31
25 mg	$120	在庫あり	Estimated Time of Arrival: December 31
50 mg	$170	在庫あり	Estimated Time of Arrival: December 31
100 mg	$240	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Guvacine hydrochloride:

Guvacine hydrobromide 在庫あり
Guvacine お問い合わせ

顧客検証

•Commun Biol. 2025 May 30;8(1):829. [Abstract]

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•関連タンパク質:

生物活性
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純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

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]

体外実験

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.

分子量

163.60

分子式

C₆H₁₀ClNO₂

CAS 番号

6027-91-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CCCNC1)O.[H]Cl

Structure Classification

Initial Source

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 25 mg/mL (152.81 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 99.93%

Select Batch:

データシート (276 KB) SDS (393 KB)

COA (248 KB) HNMR (244 KB) RP-HPLC (91 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験
^[1]

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) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[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

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
H₂O	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.