- GS967
-
- $0.00 / 1g
-
2021-10-08
- CAS:1262618-39-2
- Min. Order: 1g
- Purity: 98%
- Supply Ability: 100kgs
|
| Product Name: | GS967 | | Synonyms: | GS967;6-(4-(trifluoroMethoxy)phenyl)-3-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine;GS 458967;GS458967;GS-458967;GS-967;GS 967;GS-458967; GS 458967; GS458967;GS967(GS-458967);GS967, >98% | | CAS: | 1262618-39-2 | | MF: | C14H7F6N3O | | MW: | 347.22 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1262618-39-2.mol |  |
| | GS967 Chemical Properties |
| density | 1.52±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | insoluble in H2O; ≥13.35 mg/mL in DMSO; ≥25.52 mg/mL in EtOH with ultrasonic | | form | solid | | pka | -0.41±0.50(Predicted) |
| | GS967 Usage And Synthesis |
| Uses | GS967, also known as GS-458967, is a highly selective late sodium channel current blocker. The selective inhibition of late INa with GS967 can exert antiarrhythmic effects by suppressing EAD- and DAD-mediated extrasystolic activity in PFs and PV and SVC sleeve preparations. Selective late INa inhibition with GS967 exerts potent protective effects against ischemia-induced depolarization and repolarization abnormalities in both atria and ventricles. | | Biological Activity | gs967 is a potent, selective and novel inhibitor of cardiac late sodium current (late ina) with ic50=0.13 μm in ventricular myocytes and ic50=0.21μm in isolated hearts. [1]when na+ channels in myocytes fail to inactivate after opening, na+ influx continues throughout the ap plateau. the resulting na+ current (ina) is referred to as late ina. its magnitude is increased in many pathologic conditions, such as in the failing and/or ischemic heart, in the heart exposed to oxidative stress, and in hearts of patients with congenital long qt3 syndromes. [1]in rabbit isolated ventricular myocytes, inhibition of peak ina by gs967 is in a concentration- and voltage-dependent manner with minimal use-dependent, it also decreases the na+ and ca2+ overload. in rabbit-isolated heart, gs967 abolishes tdp induced by atx-ii or e-4031. [1]in anesthetized rabbit, gs967 reduces mapd90 but did not alter cardiac conduction time; it also prevents the induction of arrhythmic activity and tdp by clofilium and decreases the incidence of ischemia-induced arrhythmias. [1] | | references | 1. belardinelli l, liu g, smith-maxwell c et al. a novel, potent, and selective inhibitor ofcardiac late sodium current suppresses experimental arrhythmias. j pharmacol exp ther. 2013 jan;344(1):23-32. |
| | GS967 Preparation Products And Raw materials |
|