Isoguvacine hydrochloride

Name: Isoguvacine hydrochloride
Brand: MedChemExpress
SKU: HY-100810
Rating: 4.5 (1 reviews)

Cat. No.: HY-100810 Purity: 99.04%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Isoguvacine hydrochloride is a GABA receptor agonist.

For research use only. We do not sell to patients.

Isoguvacine hydrochloride Chemical Structure

CAS No. : 68547-97-7

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 26	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 26	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 24	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 36	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Isoguvacine hydrochloride is a GABA receptor agonist.

IC₅₀ & Target

GABA^[1]

In Vitro

Isoguvacine binds to a mouse forebrain synaptic membrane preparation. The specific binding is displaceable by GABA, muscimol and bicuculline but not by picrotoxin or diaminobutyric acid. Kinetic data suggest two binding affinities. Highest levels of binding are observed in the cerebellum, cortex and hippocampus^[1]. Isoguvacine binds to membrane preparations of rat forebrain with pharmacological characteristics similar to the postsynaptic GABA recognition site: that it is transported into synaptosomal preparations by an uptake system similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine is released in a Ca²⁺-dependent manner and by heteroexchange with external GABA^[2]. Isoguvacine at a concentration of 50 μM blocks the seizure like events in 2 out of 6 organotypic hippocampal slice cultures. Isoguvacine inhibits the low magnesium induced seizure like events dose dependently^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

163.60

Formula

C₆H₁₀ClNO₂

CAS No.

68547-97-7

Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CCNCC1)O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (611.25 mM; Need ultrasonic)

DMSO : 25 mg/mL (152.81 mM; Need ultrasonic; 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)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (12.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (12.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (12.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 100 mg/mL (611.25 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).

Purity & Documentation

Purity: 99.04%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (248 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Morin AM, et al. The binding of 3H-isoguvacine to mouse brain synapticmembranes. Life Sci. 1980 Apr 14;26(15):1239-45. [Content Brief]

[2]. White WF, et al. Isoguvacine binding, uptake, and release: relation to the GABA system. J Neurochem. 1983 Jun;40(6):1701-8. [Content Brief]

[3]. Wahab A, et al. Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures. Epilepsy Res. 2009 Oct;86(2-3):113-23. [Content Brief]

Kinase Assay
^[1]

The assay for ³H-Isoguvacine binding is carried out as follows: membranes suspended in Tris-citrate buffer pH 7.1 are incubated at 4°C for 10 min with 8 nM ³H-Isoguvacine. Identical samples are incubated in the presence of cold 0.5 mM GABA or 10 μM cold isoguvacine. The assay is terminated by centrifugation for 10 min at 4°C in a micro-centrifuge. The supernatants are rapidly aspirated and the surface of the pellets washed (2x) with ice-cold buffer. The pellet is resuspended in I00 μL of 0.1% Triton and placed in a scintillation vial. The assay tube is washed with I00 μL of distilled water and the wash added to the vial along with 10 ml of PCS: xylene (2:1). Counting efficiency is determined to be 40-45% in a Beckman liquid scintillation counter. Specific binding is defined as those radioactive cpm of bound ³H-Isoguvacine that are displaced by excess cold isoguvacine or GABA^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Morin AM, et al. The binding of 3H-isoguvacine to mouse brain synapticmembranes. Life Sci. 1980 Apr 14;26(15):1239-45. [Content Brief]

[2]. White WF, et al. Isoguvacine binding, uptake, and release: relation to the GABA system. J Neurochem. 1983 Jun;40(6):1701-8. [Content Brief]

[3]. Wahab A, et al. Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures. Epilepsy Res. 2009 Oct;86(2-3):113-23. [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
	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.