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

THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.

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THIP Chemical Structure

THIP Chemical Structure

CAS No. : 64603-91-4

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of THIP:

THIP Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders[1][2][3].

IC50 & Target[3]

α4β3δ GABAAR

13 μM (EC50)

In Vitro

THIP (1 µM; 5 s) induces a robust tonic GABAA-mediated current in layer 2/3 neurons[1].
THIP (1 µM; 1 s) shows no affect miniature IPSCs in layer 2/3 neurons[1].

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

THIP Related Antibodies

Cell Viability Assay[1]

Cell Line: Layer 2/3 neurons (from male postnatal day 13-19 C57BL/6 mice)
Concentration: 1 µM
Incubation Time: 5 s
Result: Induced a tonic current of 43.2 pA.

Cell Viability Assay[1]

Cell Line: Layer 2/3 neurons (from male postnatal day 13-19 C57BL/6 mice)
Concentration: 1 µM
Incubation Time: 1 s
Result: Resulted in only minor changes in the amplitude and frequency of mIPSCs.
In Vivo

THIP (Gaboxadol) (0.5, 5.0 mg/kg; p.o.; single) shws a good oral utilization, with Fa values of 110% and 83% for dosage of 0.5 and 5.0 mg/kg, respectively[2].

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

Animal Model: Sprague-Dawley rats (255-276 g)[2].
Dosage: 2.5 mg/kg (for i.v.); 0.5 and 5.0 mg/kg (for p.o.).
Administration: Oral gavage; intravenous injection; single.
Result: 1.19 Pharmacokinetic Parameters of THIP 4 in Sprague-Dawley rats[2].
IV (2.5 mg/kg) PO (0.5 mg/kg) PO (5.0 mg/kg)
AUC (ng/mL•h) 1193 263 1988
Tmax (h) - 0.22 0.33
Cmax (ng/mL) 4350 291 2061
CL/Fa (mL/h/kg) - 1939 2558
CL (mL/h/kg) 2043 - -
Fa (%) 100 110 83
Clinical Trial
Molecular Weight

140.14

Formula

C6H8N2O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1C2=C(CNCC2)ON1
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 : 50 mg/mL (356.79 mM; ultrasonic and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 23.33 mg/mL (166.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 7.1357 mL 35.6786 mL 71.3572 mL
5 mM 1.4271 mL 7.1357 mL 14.2714 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. 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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: ≥ 2.5 mg/mL (17.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (17.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 50 mg/mL (356.79 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).
Purity & Documentation

Purity: 99.93%

COA (249 KB) HNMR (241 KB) RP-HPLC (275 KB) MS (69 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. 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
H2O / DMSO 1 mM 7.1357 mL 35.6786 mL 71.3572 mL 178.3930 mL
5 mM 1.4271 mL 7.1357 mL 14.2714 mL 35.6786 mL
10 mM 0.7136 mL 3.5679 mL 7.1357 mL 17.8393 mL
15 mM 0.4757 mL 2.3786 mL 4.7571 mL 11.8929 mL
20 mM 0.3568 mL 1.7839 mL 3.5679 mL 8.9197 mL
25 mM 0.2854 mL 1.4271 mL 2.8543 mL 7.1357 mL
30 mM 0.2379 mL 1.1893 mL 2.3786 mL 5.9464 mL
40 mM 0.1784 mL 0.8920 mL 1.7839 mL 4.4598 mL
50 mM 0.1427 mL 0.7136 mL 1.4271 mL 3.5679 mL
60 mM 0.1189 mL 0.5946 mL 1.1893 mL 2.9732 mL
80 mM 0.0892 mL 0.4460 mL 0.8920 mL 2.2299 mL
100 mM 0.0714 mL 0.3568 mL 0.7136 mL 1.7839 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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THIP 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:

THIP64603-91-4GaboxadolGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorIPSCssleep disordersneuronsInhibitorinhibitorinhibit

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