A KCC2 cotransporter activator
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Pro-drug Form(s)
31448CLP 290
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CLP 257

Item No. 30948

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(5Z)-5-[(4-fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1(2H)-pyridazinyl)-4(5H)-thiazolone
CAS Number
1181081-71-9
Molecular Formula
C14H14FN3O2S
Formula Weight
307.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 20 mg/ml
SMILES
FC1=CC=C(/C=C2SC(N3NCCCC3)=NC\2=O)C(O)=C1
InChi Code
InChI=1S/C14H14FN3O2S/c15-10-4-3-9(11(19)8-10)7-12-13(20)17-14(21-12)18-6-2-1-5-16-18/h3-4,7-8,16,19H,1-2,5-6H2/b12-7-
InChi Key
SKCADXVKQRCWTR-GHXNOFRVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    Product Description

    CLP 257 is a K+/Cl- cotransporter 2 (KCC2) activator.1,2,3 It induces chloride transport in NG108-cl cells that endogenously express low levels of KCC2 (EC50 = 616 nM).1 It is selective for KCC2 over GABAA receptors at 50 µM. CLP 257 (25 µM) increases the rate of chloride accumulation in spinal slices isolated from a rat model of peripheral nerve injury and BDNF control slices, which exhibit reduced levels of KCC2. In vivo, CLP 257 (100 mg/kg) increases mechanical and withdrawal thresholds in a rat model of peripheral nerve injury and reverses morphine-induced hyperalgesia in rats.1,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gagnon, M., Bergeron, M.J., Lavertu, G., et al. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat. Med. 19(11), 1524-1528 (2013).

    2. Cardarelli, R.A., Jones, K., Pisella, L.I., et al. The small molecule CLP257 does not modify activity of the K+-Cl- co-tansporter KCC2 but does potentiate GABAA receptor activity. Nat. Med. 23(12), 1394-1396 (2017).

    3. Gagnon, M., Bergeron, M.J., Perez-Sanchez, J., et al. Reply to The small molecule CLP257 does not modify activity of the K+-Cl- co-transporter KCC2 but does potentiate GABAA receptor activity. Nat. Med. 23(12), 1396-1398 (2017).

    4. Ferrini, F., Lorenzo, L.-E., Godin, A.G., et al. Enhancing KCC2 function counteracts morphine-induced hyperalgesia. Sci. Rep. 7(1), 3870 (2017).