An ion channel modulator
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NS 3623

Item No. 34992

Technical Information
Formal Name
N-[4-bromo-2-(2H-tetrazol-5-yl)phenyl]-N′-[3-(trifluoromethyl)phenyl]-urea
CAS Number
343630-41-1
Molecular Formula
C15H10BrF3N6O
Formula Weight
Purity
≥95%
Formulation
A solid
DMF: 5 mg/mlDMSO: 1 mg/mlEthanol: 2 mg/mlPBS (pH 7.2): insol
λmax
227, 245, 271, 381 nm
SMILES
O=C(NC1=C(C2=NN=NN2)C=C(Br)C=C1)NC3=CC=CC(C(F)(F)F)=C3
InChi Code
InChI=1S/C15H10BrF3N6O/c16-9-4-5-12(11(7-9)13-22-24-25-23-13)21-14(26)20-10-3-1-2-8(6-10)15(17,18)19/h1-7H,(H2,20,21,26)(H,22,23,24,25)
InChi Key
JXPULDIATMTIIN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NS 3623 is an ion channel modulator.1,2,3 It inhibits the volume-regulated anion channel (VRAC) in HEK293 cells and chloride conductance in isolated human red blood cells (IC50s = 1.8 and 0.21 µM, respectively).1,2 NS 3623 also activates human-ether-a-go-go (hERG), also known as Kv11.1 (EC50 = 79.4 µM) but does not activate the voltage-gated potassium channel (Kv) subtypes Kv1.5, Kv4.3, or Kv7.1 at 30 µM.3 It increases red blood cell density and improves red blood cell morphology in the SAD transgenic mouse model of sickle cell disease when administered at a dose of 100 mg/kg per day for 21 days.2 NS 3623 (50 mg/kg) reverses QT interval prolongation induced by the hERG inhibitor E-4031 (Item No. 15203) in conscious guinea pigs.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hélix, D., Strøbaek, B.H.D., and Christophersen, P. Inhibition of the endogenous volume-regulated anion channel (VRAC) in HEK293 cells by acidic di-aryl-ureas. J. Membr. Biol. 196(2), 83-94 (2003).

    2. Bennekou, P., de Franceschi, L., Pedersen, O., et alTreatment with NS3623, a novel Cl-conductance blocker, ameliorates erythrocyte dehydration in transgenic SAD mice: a possible new therapeutic approach for sickle cell disease. Blood 97(5), 1451-1457 (2001).

    3. Hansen, R.S., Diness, T.G., Christ, T., et alBiophysical characterization of the new human ether-a-go-go-related gene channel opener NS3623 [N-(4-bromo-2-(1H-tetrazol-5-yl)-phenyl)-N'-(3'-trifluoromethylphenyl)urea]. Mol. Pharmacol. 70(4), 1319-1329 (2006).

    4. Hansen, R.S., Olesen, S.-P., Rønn, L.C.B., et alIn vivo effects of the IKr agonist NS3623 on cardiac electrophysiology of the guinea pig. J. Cardiovasc. Pharmacol. 52(1), 35-41 (2008).