GS967 Sodium Channel inhibitor

Jump to

Quality Control

Batch: S527401 Ethanol]46 mg/mL]false]DMSO]45 mg/mL]false]Water]Insoluble]false Purity: 99.98%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.98

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other Sodium Channel Inhibitors	Camostat Mesilate A-803467 cariporide Tolperisone HCl Vinpocetine Veratramine Bulleyaconi cine A Ambroxol HCl Benzocaine Nefopam HCl

Chemical Information, Storage & Stability

Molecular Weight	347.22	Formula	C₁₄H₇F₆N₃O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1262618-39-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GS458967			Smiles	C1=CC(=CC=C1C2=CN3C(=NN=C3C(F)(F)F)C=C2)OC(F)(F)F

Solubility

In vitro
Batch:

Ethanol : 46 mg/mL

DMSO : 45 mg/mL (129.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	late INa 0.13 μM
In vitro	GS967 (3 μM) has no significant effect on L- or T-type calcium channel currents or Na+-Ca2+ exchanger current (INCX), and 1 μM of this compound has minimal or no effect on the ATP-inhibited K+ current or on human cardiac ion channels expressed in human embryonic kidney 293 or Chinese hamster ovary cells. This compound is a novel Sodium Channel modulator specifically developed to inhibit persistent sodium current, with a 42-fold preference for persistent as opposed to peak current inhibition.
In vivo	GS967 protects against seizures and premature lethality in vivo. Chronic administration of this compound does not cause overt behavioural toxicity or sedation in wild-type mice at the effective anticonvulsant dose. It suppresses arrhythmogenicity evoked by ischaemia, hypokalaemia, and catecholamines in canine and porcine models
References	[1] https://pubmed.ncbi.nlm.nih.gov/23010360/ [2] https://pubmed.ncbi.nlm.nih.gov/29782051/ [3] https://pubmed.ncbi.nlm.nih.gov/27136942/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Chemical Structure

Molecular Weight: 347.22