| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized Powder |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Soluble in DMSO.It is recommended to prepare fresh solutions before use. Centrifuge all products before use (10000 x, g 5 min). Avoid multiple freezing and thawing. |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: (6-[4-(trifluoromethoxy)phenyl]-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine)
- Also known as: 6-(4-(Trifluoromethoxy)phenyl)-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine, GS-458967, GS-961, 1262618-39-2
- CAS number: 1262618-39-2
- Molecular formula: C14H7F6N3O
- Purity: >99%
- Concentration: 0.1 - 10 µM
- Form: Lyophilized Powder
- Solubility: Soluble in DMSO.It is recommended to prepare fresh solutions before use. Centrifuge all products before use (10000 x, g 5 min). Avoid multiple freezing and thawing.
- Reconstitution: Soluble in DMSO.It is recommended to prepare fresh solutions before use. Centrifuge all products before use (10000 x, g 5 min). Avoid multiple freezing and thawing.
- 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: Late INa, Nav 1.5
- Source: Synthetic
- Activity: A potent and selective inhibitor of cardiac late sodium current (INa), that has been shown to suppress ventricular arrhythmias1. GS967 inhibited Anemonia sulcata toxin II (ATX-II)-induced late INa in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21 µM, respectively1.
- Alternative names: 6-(4-(Trifluoromethoxy)phenyl)-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine, GS-458967, GS-961, 1262618-39-2
Scientific background
Voltage-gated sodium (NaV) channels are integral membrane proteins that play an essential role in the regulation of action potentials in neurons, myocytes and endocrine cells1. Given their central role in electrical signaling, NaVs inhibitors have been extensively studied. Inhibitors of Navs have been found to be highly effective as local anesthetics, anticonvulsants and antiarrhythmic and in the prevention of myocardial ischemia and heart failure2. Late Na+ current (INaL) is a phenomenon that occurs when NaVs in myocytes fail to regulate Na+ influx. Increased magnitude of late INaL is associated with pathological conditions. Inhibition of cardiac late INa is a strategy to suppress arrhythmias and Na+-dependent calcium overload associated with myocardial ischemia and heart failure3. GS967 is a potent and selective inhibitor of late INa. It was shown to inhibit ATX-II (#STA-700) induced late INa in ventricular myocytes and isolated hearts4-5. Photogenic variant SCN8A, encoding the NaV α subunit Nav1.6, is a known cause of epilepsy. Treatment of mice carrying the SCN8A mutation with G967 resulted in lower seizure burden and complete protection from seizure-associated lethality6.
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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