[CAS NO. 85118-33-8] Gaboxadol hydrochloride

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PRODUCTS SPECIFICATIONS [85118-33-8]

Catalog

HY-10233

Brand

MCE

CAS

85118-33-8

DESCRIPTION [85118-33-8]

Overview

MDL	MFCD00055180
Molecular Weight	176.60
Molecular Formula	C6H9ClN2O2
SMILES	O=C1C2=C(CNCC2)ON1.Cl

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

1 Publications Citing Use of MCE

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

Summary

Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABA _A receptor and an antagonist of GABA _C receptors ( IC ₅₀ =25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED ₅₀ value of 143 µM, a full agonist efficacy at α5 subunit ( ED ₅₀ =28-129 µM) and a superagonist efficacy at α4β3δ ( ED ₅₀ =6 µM). Gaboxadol hydrochloride is a non-opioid agent ^[1] ^[2] .

IC50 & Target

GABA _A receptor; GABA _C 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 P _app 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] .

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

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] .

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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00266357	H. Lundbeck A+S	Primary Insomnia	November 2005	Phase 2
NCT00094666	H. Lundbeck A+S	Primary Insomnia	November 2004	Phase 3
NCT00094627	H. Lundbeck A+S	Primary Insomnia	November 2004	Phase 3
NCT00095069	H. Lundbeck A+S	Insomnia	October 2004	Phase 3
NCT03697161	Ovid Therapeutics Inc.	Fragile X Syndrome (FXS)	September 17, 2018	Phase 2
NCT00209963	H. Lundbeck A+S	Primary Insomnia	June 2003	Phase 3
NCT00209937	H. Lundbeck A+S	Primary Insomnia	January 2003	Phase 3
NCT00095043	H. Lundbeck A+S	Insomnia	October 2004	Phase 3
NCT00266344	H. Lundbeck A+S	Primary Insomnia	November 2005	Phase 2
NCT00102167	H. Lundbeck A+S	Insomnia	February 2005	Phase 3
NCT00807248	H. Lundbeck A+S	Major Depressive Disorder	November 2008	Phase 2
NCT00209950	H. Lundbeck A+S	Primary Insomnia	July 2004	Phase 3
NCT00209846	H. Lundbeck A+S	Primary Insomnia	June 2004	Phase 3
NCT04106557	Ovid Therapeutics Inc.	Primary Disease or Condition Being Studied: Angelman Syndrome (AS)	September 9, 2019	Phase 3
NCT00103818	H. Lundbeck A+S	Insomnia	February 2005	Phase 3
NCT00209924	H. Lundbeck A+S	Primary Insomnia	April 2004	Phase 3
NCT00102154	H. Lundbeck A+S	Insomnia	January 2005	Phase 3
NCT04823052	Healx Limited	Fragile X Syndrome	May 25, 2022	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

H ₂ O : ≥ 100 mg/mL ( 566.25 mM )

DMSO : 75 mg/mL ( 424.69 mM ; Need ultrasonic)

* "≥" 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
10 mM	0.5663 mL	2.8313 mL	5.6625 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 100 mg/mL (566.25 mM); Clear solution; Need ultrasonic
2.

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
3.

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
4.

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

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

* All of the co-solvents are available by MCE.

References

Synonyms

Isoxazolo[5,4-c]pyridin-3(2H)-one, 4,5,6,7-tetrahydro-, hydrochloride (1:1)

Isoxazolo[5,4-c]pyridin-3(2H)-one, 4,5,6,7-tetrahydro-, monohydrochloride

Gaboxadol hydrochloride

4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrochloride

THIP hydrochloride