| Identification | Back Directory | [Name]
THIP HYDROCHLORIDE | [CAS]
64603-91-4 | [Synonyms]
THIP
THPO
gaboxadol
Lu 02-030
Gaboxadolum
Einecs 264-963-0
THIP HYDROCHLORIDE
Gaboxadolum [latin]
4,5,6,7-TETRAHYDROISOXAZOLO[5,4-C]PYRIDIN-3-OL
4,5,6,7-Tetrahydroisoxazole(5,4-C)pyridin-3-ol
4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3(2H)-one
Isoxazolo(5,4-C)pyridin-3(2H)-one, 4,5,6,7-tetrahydro-
Recombinant Mouse Thrombopoietin/Tpo/Thpo Protein, His Tag
4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3(2h)-onehydrate
4-c)pyridin-3(2h)-one,4,5,6,7-tetrahydro-isoxazolo(hydrate
4,5,6,7-TETRAHYDROISOXAZOLO[5,4-C]PYRIDIN-3-OL HYDROCHLORIDE
4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3(2H)-one hydrochloride | [EINECS(EC#)]
264-963-0 | [Molecular Formula]
C6H8N2O2 | [MDL Number]
MFCD00055180 | [MOL File]
64603-91-4.mol | [Molecular Weight]
140.14 |
| Chemical Properties | Back Directory | [Melting point ]
242-244° (dec) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
ethanol: 0.91 mg/mL
| [form ]
solid
| [pka]
pKa (water, 25°): 4.44 ±0.03; 8.48 ±0.04 | [color ]
white
| [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
Gaboxadol HCl (64603-91-4) is a GABA-A receptor agonist. Hypnotic agent. | [Uses]
GABAa agonist, GABAc antagonist | [Definition]
ChEBI: 4,5,6,7-Tetrahydroisoxazolo(5,4-c)pyridin-3-ol is an oxazole. | [Biological Activity]
Systemically active GABA A receptor agonist and GABA C receptor antagonist. Displays antinociceptive, anticonvulsant and sedative effects. Hypnotic agent that enhances delta activity within non-REM sleep in rats. | [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]. | 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: | 1.19Pharmacokinetic 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 |
|
| [IC 50]
α4β3δ GABAAR: 13 μM (EC50) | [storage]
Store at -20°C | [References]
1) Meera et al. (2011), Molecular basis for the high THIP/gaboxadol sensitivity of extrasynaptic GABA(A) receptors; J. Neurophysiol., 106 2057 |
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| Company Name: |
Xi'an MC Biotech, Co., Ltd.
|
| Telephone: |
029-89275612 +8618991951683 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList1759320/0_EN.htm |
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