{"product_id":"gaba-a-compound-1b-bhb21300109","title":"GABA(A)-Compound 1b","description":"\u003ch3\u003eProduct details\u003c\/h3\u003e \u003cul\u003e\n\u003cli\u003e\n\u003cstrong\u003eChemical name:\u003c\/strong\u003e 8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eAlso known as:\u003c\/strong\u003e 8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003ePubChem CID:\u003c\/strong\u003e 136118605\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eMolecular formula:\u003c\/strong\u003e C20H12F3N3O2S.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003ePurity:\u003c\/strong\u003e \u0026gt;98% (HPLC)\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eConcentration:\u003c\/strong\u003e 0.1-10 µM.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eForm:\u003c\/strong\u003e Lyophilized powder.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eSolubility:\u003c\/strong\u003e Soluble in DMSO. Centrifuge before use (10000 x g, 5 min).\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eReconstitution:\u003c\/strong\u003e 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\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eShipping:\u003c\/strong\u003e 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.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eTarget:\u003c\/strong\u003e GABA(A) receptors\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eSource:\u003c\/strong\u003e Synthetic\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eActivity:\u003c\/strong\u003e 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, \u0026gt;10, 0.48 and 0.91 µM, respectively)1.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eAlternative names:\u003c\/strong\u003e 8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one\u003c\/li\u003e\n\u003c\/ul\u003e \u003ch3\u003eScientific background\u003c\/h3\u003e \u003cp\u003eGABA(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.\u003c\/p\u003e \u003cp\u003e\u003cstrong\u003eLead time:\u003c\/strong\u003e 1-2 Business Days\u003c\/p\u003e \u003cp\u003e\u003cstrong\u003eCountry of origin:\u003c\/strong\u003e Israel\/IL\u003c\/p\u003e \u003ch3\u003eApplications key\u003c\/h3\u003e \u003cp\u003eApplication key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.\u003c\/p\u003e \u003cp\u003e\u003cstrong\u003eBioassay tested:\u003c\/strong\u003e Yes\u003c\/p\u003e","brand":"Alomone Labs","offers":[{"title":"10 mg \/ 1","offer_id":53249706623341,"sku":"CMG-004-10MG-1","price":509.0,"currency_code":"USD","in_stock":true},{"title":"25 mg \/ 1","offer_id":53311555961197,"sku":"CMG-004-25MG-1","price":1019.0,"currency_code":"USD","in_stock":true},{"title":"5 mg \/ 1","offer_id":53311555993965,"sku":"CMG-004-5MG-1","price":287.0,"currency_code":"USD","in_stock":true},{"title":"50 mg \/ 1","offer_id":53311556026733,"sku":"CMG-004-50MG-1","price":1648.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/CMG-004_gr.gif?v=1778544414","url":"https:\/\/www.ebiohippo.com\/products\/gaba-a-compound-1b-bhb21300109","provider":"BioHippo","version":"1.0","type":"link"}