GABAA-compound 1b

ArtNr	ALO-CMG-004-5mg
Hersteller	Alomone
Menge	5 mg
Quantity options	10 mg 25 mg 50 mg 5 mg
Kategorie	Neuroscience Molecular Targets for Neuroscience Targets for Rodent Neurosciences Neural Signaling Reagents & Chemicals Molecules
Typ	Small Molecules
Format	Lyophilized
Specific against	other
Purity	>98% (HPLC)
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Versandbedingung	Raumtemperatur
Lieferbar
Manufacturer - Type	Non Antibodies
Manufacturer - Category	S. Molecules
Manufacturer - Targets	GABA(A) receptors
Country of Origin	Israel
Shipping Temperature	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Storage Conditions	Storage as Solution: Up to three months at -20°C. - Storage before Reconstitution: The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture. - Storage after Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.
Molecular Weight	415, 39
Manufacturer - Format	Lyophilized powder.
Short description	A Novel Antagonist of GABA(A) Receptors
Description	8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1, 9-dihydro-2H-[1, 3]oxazolo[4, 5-h][2, 3]benzodiazepin-2-one - A Novel Antagonist of GABA(A) Receptors
Reconstitution	Centrifuge the vial before adding solvent (10, 000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
PH	7, 4
UNSPSC	41116134
CID	136118605
Effective Concentration	0.1-10 µM.
Activity	A novel antagonist of α5 containing GABA(A) receptors, displaying significant selectivity for α5 (IC50 = 201 nM, Imax = 92%) over α1, α2, α3 and α4 containing receptors, on which it produces only partial maximum inhibition (Imax = 54, 0, 39 and 35%, respectively) at higher concentrations (IC50 = 0.48, >10, 0.48 and 0.91 µM, respectively)1.
Solubility	Soluble in DMSO. Centrifuge before use (10000 x g, 5 min).
Bioassay tested	Yes
Chemical Name	8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1, 9-dihydro-2H-[1, 3]oxazolo[4, 5-h][2, 3]benzodiazepin-2-one.
Scientific Background	GABA(A)-Compound 1b (8-methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1, 9-dihydro-2H-[1, 3]oxazolo[4, 5-h][2, 3]benzodiazepin-2-one) is a potent and selective antagonist of α5 containing GABA(A) receptors, displaying an IC50 value of 201 nM. On α1-4 containing receptors, the antagonist demonstrates only partial maximum inhibition1.GABA(A)-Compound 1b is characterized as a 2, 3-benzodiazepine with substantial blood-brain barrier permeability. In vivo studies reveal that 1b is devoid of sedative effects, is pro-convulsive, and enhances the performance of rats in the object recognition test.GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA action, a major inhibitory neurotransmitter throughout the central nervous system (CNS), thus play an important role in inhibiting cell excitation in the CNS.GABA(A) receptors are considered a major target of antiseizure drugs2.

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ALO-CMG-004-5mg-safety-datasheet.pdf