1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. Isoguvacine hydrochloride

Isoguvacine hydrochloride 

Cat. No.: HY-100810 Purity: 98.80%
Handling Instructions

Isoguvacine hydrochloride is a GABA receptor agonist.

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

Isoguvacine hydrochloride Chemical Structure

Isoguvacine hydrochloride Chemical Structure

CAS No. : 68547-97-7

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10 mM * 1 mL in DMSO USD 79 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (12.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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

Purity: 98.80%

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Keywords:

IsoguvacineGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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Product Name:
Isoguvacine hydrochloride
Cat. No.:
HY-100810
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