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CLP257

  Cat. No.:  DC11507   Featured
Chemical Structure
1181081-71-9
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More than 5000 active chemicals with high quality for research!
Field of application
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 i
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1181081-71-9
Chemical Name: (5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone
Synonyms: CLP-257
SMILES: S1/C(=C\C2=CC=C(F)C=C2O)/C(=O)N=C1N1NCCCC1
Formula: C14H14FN3O2S
M.Wt: 307.34
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 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.
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 Vivo: CLP257 (100 mg/kg; intraperitoneal injection; adult male rats) treatment induced a significant increase in mechanical sensitivity[2]. Animal Model: Adult male rats (300 g) injected with Morphine[2] Dosage: 100 mg/kg Administration: Intraperitoneal injection Result: Induced a significant increase in mechanical sensitivity.
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[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC11507 CLP257 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 i
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