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Home / Biochemicals / Small Molecules

GS967

SKU : BHB21300161

A potent and selective blocker of cardiac late sodium channel (late I(Na)).

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Alomone Labs

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Mfr.No.	G-225, G-225_25 mg, G-225_250 mg, G-225_50 mg
Description	GS967 (#G-225) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C14H7F6N3O
Synonyms	Synthetic
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 alpha 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.
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
Concentration	0.1 - 10 uM
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.
Cas Number	1262618-39-2
Molecular Weight	347.2
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.
Target	Late INa, Nav 1.5
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 uM, respectively1.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: (6-(4-(trifluoromethoxy)phenyl)-3-(trifluoromethyl)-(1,2,4)triazolo(4,3-a)pyridine)

Purity	>99%
Form	Lyophilized Powder
Storage	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. Storage of solutions: Store up to four weeks at 4°C or three months at -20°C.

Product Manual	SDS

Reference	Yu, F.H. et al. (2003) Gen. Biol., 4, 207. Mulcahy, V. et al. (2019) J. Med. Chem., 62, 8695. Makielski, J.C. (2009) J. Cardiovasc. Pharmacol., 54, 279. Belardinelli, L. et al. (2013) J. Pharmacol. Exp. Ther., 344, 23. Del Canto, I. et al. (2018) Cardiovasc. Drugs. Ther., 32, 413. Baker, M.E. et al. (2018) Epilepsia. 59, 1166. Belardinelli, L., et al. (2013) J. Pharmacol. Exp. Ther. 344, 23.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300161-1	G-225_25 mg	25 mg	$140		Add to Cart
BHB21300161-2	G-225_250 mg	250 mg	$588		Add to Cart
BHB21300161-3	G-225_50 mg	50 mg	$198		Add to Cart

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