THIP (Synonyms: Gaboxadol)

Name: THIP
Brand: MedChemExpress
SKU: HY-10232
Rating: 4.5 (1 reviews)

Cat. No.: HY-10232 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

THIP Chemical Structure

CAS No. : 64603-91-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 32	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 145	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of THIP:

THIP-d₄ Get quote
Gaboxadol hydrochloride Get quote

1 Publications Citing Use of MCE THIP

•Can J Physiol Pharmacol. 2020 Oct;98(10):725-732. [Abstract]

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Biological Activity
Purity & Documentation
References
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Description

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.

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 F_a 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
T_max (h)	-	0.22	0.33
C_max (ng/mL)	4350	291	2061
CL/F_a (mL/h/kg)	-	1939	2558
CL (mL/h/kg)	2043	-	-
F_a (%)	100	110	83

Clinical Trial

Molecular Weight

140.14

Formula

C₆H₈N₂O₂

CAS No.

64603-91-4

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
10 mM	0.7136 mL	3.5679 mL	7.1357 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (14.84 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.

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)

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%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (249 KB) HNMR (241 KB) RP-HPLC (275 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Drasbek KR, et al. THIP, a hypnotic and antinociceptive drug, enhances an extrasynaptic GABAA receptor-mediated conductance in mouse neocortex. Cereb Cortex. 2006 Aug;16(8):1134-41. [Content Brief]

[2]. Larsen M, et al. 5-Hydroxy-L-tryptophan alters gaboxadol pharmacokinetics in rats: involvement of PAT1 and rOat1 in gaboxadol absorption and elimination. Eur J Pharm Sci. 2010 Jan 31;39(1-3):68-75. [Content Brief]

[3]. Hoestgaard-Jensen K, et al. Probing α4βδ GABAA receptor heterogeneity: differential regional effects of a functionally selective α4β1δ/α4β3δ receptor agonist on tonic and phasic inhibition in rat brain. J Neurosci. 2014 Dec 3;34(49):16256-72. [Content Brief]

Complete Stock Solution Preparation Table

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.

THIP Related Classifications

Neurological Disease

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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THIP (Synonyms: Gaboxadol)

Customer Review

Other Forms of THIP:

THIP Related Antibodies

1 Publications Citing Use of MCE THIP

Featured Recommendations

•Related Screening Libraries:

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•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

THIP Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

THIP Related Classifications

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