CLP257( CLP-257 )

Catalog No. M10616 CAS No. 1181081-71-9

CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM.

Purity : >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

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Biological Information

Product Name

CLP257
Note

Research use only, not for human use.
Brief Description

CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM.
Description

CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM; displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors; restores impaired Cl(-) transport in neurons, rescues KCC2 plasma membrane expression; renormalizes stimulus-evoked responses in spinal nociceptive pathways in a rat model of neuropathic pain.
In Vitro

There is no change in [Cl?]i in HEK293-cl cells when incubated with CLP257, indicating inactivity on NKCC1, KCC1, KCC3 or KCC4. Oocyte pre-incubation with CLP257 (200 nM) increases KCC2 transport activity by 61%, but causes no change in other CCCs. Functional, dose-dependent antagonism is also observed between CLP257 and the recently characterized KCC2 antagonist VU024055119. CLP257 (50 μM) provokes < 0.2% of the effect of 5 μM muscimol in CHO cells transduced with recombinant α1β2γ2 GABAA receptors, indicating negligible agonist activity of CLP257 on GABAA receptors.
In Vivo

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Synonyms

CLP-257
Pathway

Membrane Transporter/Ion Channel
Target

Chloride Channel
Recptor

Chloride Channel
Research Area

——
Indication

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Chemical Information

CAS Number

1181081-71-9
Formula Weight

307.34
Molecular Formula

C14H14FN3O2S
Purity

>98% (HPLC)
Solubility

100 mM in DMSO
SMILES

O=C1N=C(N2CCCCN2)S/C1=C\C3=CC=C(F)C=C3O
Chemical Name

(5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. Cardarelli RA, et al. Nat Med. 2017 Dec 7;23(12):1394-1396. 2. Gagnon M, et al. Nat Med. 2013 Nov;19(11):1524-8. 3. Ferrini F, et al. Sci Rep. 2017 Jun 20;7(1):3870.

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