A KCC2 cotransporter inhibitor
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VU0240551

Item No. 29790

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-acetamide
CAS Number
893990-34-6
Molecular Formula
C16H14N4OS2
Formula Weight
342.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
277 nm
SMILES
O=C(NC1=NC(C)=CS1)CSC(N=N2)=CC=C2C3=CC=CC=C3
InChi Code
InChI=1S/C16H14N4OS2/c1-11-9-23-16(17-11)18-14(21)10-22-15-8-7-13(19-20-15)12-5-3-2-4-6-12/h2-9H,10H2,1H3,(H,17,18,21)
InChi Key
WJRWSLORVIHRNX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $86

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    10 mg

    $146

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    25 mg

    $321

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    50 mg

    $598

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    Product Description

    VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM).1 It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 µM) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 µM. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Delpire, E., Days, E., Lewis, L.M., et al. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc. Natl. Acad. Sci. USA 106(13), 5383-5388 (2009).