Description
Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP 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 analgesic and has hypnotic activities.
Product information
CAS Number: 85118-33-8
Molecular Weight: 176.60
Formula: C6H9ClN2O2
Chemical Name: 2H,3H,4H,5H,6H,7H-[1,2]oxazolo[5,4-c]pyridin-3-one hydrochloride
Smiles: Cl.O=C1NOC2CNCCC=21
InChiKey: ZDZDSZQYRBZPNN-UHFFFAOYSA-N
InChi: InChI=1S/C6H8N2O2.ClH/c9-6-4-1-2-7-3-5(4)10-8-6;/h7H,1-3H2,(H,8,9);1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 75 mg/mL (424.69 mM; Need ultrasonic). H2O : ≥ 100 mg/mL (566.25 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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