2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Gaboxadol hydrochloride

Gaboxadol hydrochloride  (Synonyms: Lu 02-030 hydrochloride; THIP hydrochloride)

Cat. No.: HY-10233 Purity: 99.85%
COA
SDS
Handling Instructions Technical Support

Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent.

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Gaboxadol hydrochloride

Gaboxadol hydrochloride 화학구조

CAS No. : 85118-33-8

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 1 publication(s) in Google Scholar

Other Forms of Gaboxadol hydrochloride:

Gaboxadol hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Gaboxadol hydrochloride

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent[1][2].

IC50 & Target

GABAA receptor; GABAC receptor[1]
In Vitro

Gaboxadol hydrochloride (0.34, 3.5 and 7.0 μM) decreses permeability across Caco-2 cell monolayers with a dose dependent manner, shows the mean Papp values with 8.1 × 10-6 cm·s-1, 6.1 × 10-1 cm·s-6 and 5.6 × 10-6 cm·s-1 for 0.34, 3.5 and 7 μM gaboxadol, respectively[3].

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

Gaboxadol hydrochloride Related Antibodies
In Vivo

Gaboxadol hydrochloride (intraperitoneal injection; 0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg; once daily; three-day interval) normalizes the distance traveled by Fmr1 KO2 mice to WT activity levels at 0.5 mg/kg, additionally, this compound has no effect on locomotor activity in Fmr1 KO2 mice[2].

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

Animal Model: Fmr1 KO2 mice (deletion of the promoter and first exon of Fmr1 resulting in mRNA and protein null mice)[2]
Dosage: 0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg
Administration: Intraperitoneal injection
Result: Normalized Hyperactivity Observed in Fmr1 KO2 mice.
Clinical Trial
분자량

176.60

화학식

C6H9ClN2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(CNCC2)ON1.Cl
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture and light

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

용액&용해도
In Vitro: 

H2O : ≥ 100 mg/mL (566.25 mM)

DMSO : 75 mg/mL (424.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.6625 mL 28.3126 mL 56.6251 mL
5 mM 1.1325 mL 5.6625 mL 11.3250 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 and light). 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 1.47 mg/mL (8.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.47 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.7 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: ≥ 1.47 mg/mL (8.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.47 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.7 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.

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 (566.25 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
순도&문서

Purity: 99.85%

SDS (394 KB)

COA (252 KB) HNMR (245 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 5.6625 mL 28.3126 mL 56.6251 mL 141.5628 mL
5 mM 1.1325 mL 5.6625 mL 11.3250 mL 28.3126 mL
10 mM 0.5663 mL 2.8313 mL 5.6625 mL 14.1563 mL
15 mM 0.3775 mL 1.8875 mL 3.7750 mL 9.4375 mL
20 mM 0.2831 mL 1.4156 mL 2.8313 mL 7.0781 mL
25 mM 0.2265 mL 1.1325 mL 2.2650 mL 5.6625 mL
30 mM 0.1888 mL 0.9438 mL 1.8875 mL 4.7188 mL
40 mM 0.1416 mL 0.7078 mL 1.4156 mL 3.5391 mL
50 mM 0.1133 mL 0.5663 mL 1.1325 mL 2.8313 mL
60 mM 0.0944 mL 0.4719 mL 0.9438 mL 2.3594 mL
80 mM 0.0708 mL 0.3539 mL 0.7078 mL 1.7695 mL
100 mM 0.0566 mL 0.2831 mL 0.5663 mL 1.4156 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.

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Gaboxadol hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gaboxadol85118-33-8Lu 02-030THIPGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorGABAAGABACnon-opioidanalgesichypnoticsleepInhibitorinhibitorinhibit

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상품명:
Gaboxadol hydrochloride
Cat. No.:
HY-10233
수량:
MCE Japan Authorized Agent:

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