| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Soluble in DMSO. Centrifuge before use (10000 x g, 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- 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.
- Also known as: 8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one
- PubChem CID: 136118605
- Molecular formula: C20H12F3N3O2S.
- Purity: >98% (HPLC)
- Concentration: 0.1-10 µM.
- Form: Lyophilized powder.
- Solubility: Soluble in DMSO. Centrifuge before use (10000 x g, 5 min).
- 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
- Shipping: 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.
- Target: GABA(A) receptors
- Source: Synthetic
- 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.
- Alternative names: 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.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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