CLP-290

  Cat. No.:  DC12714   Featured
Chemical Structure
1181083-81-7
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More than 5000 active chemicals with high quality for research!
Field of application
CLP290 (CLP-290) is an orally acirtve small molecule K+-Cl- cotransporter isotype 2 (KCC2) activator, the carbamate prodrug of CLP257; In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in SDH neurons. Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior.
Cas No.: 1181083-81-7
Chemical Name: [5-Fluoro-2-[(Z)-(2-hexahydropyridazin-1-yl-4-oxo-thiazol-5-ylidene)methyl]phenyl] pyrrolidine-1-carboxylate
Synonyms: CLP-290,CLP 290,CLP290
SMILES: N(C(OC1=CC(F)=CC=C1/C=C1\SC(N2NCCCC2)=NC\1=O)=O)1CCCC1
Formula: C19H21FN4O3S
M.Wt: 404.46
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Chen B, et al. Cell. 2018 Jul 26;174(3):521-535.e13. 2. Ferrini F, et al. Sci Rep. 2017 Jun 20;7(1):3870.
Description: CLP290 is an orally available activator of the neuron-specific K+-Cl− cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats[1][2].
Target: KCC2[1]
References: [1]. Ferrini F, et al. Enhancing KCC2 function counteracts morphine-induced hyperalgesia. Sci Rep. 2017 Jun 20;7(1):3870. [2]. Gagnon M, et al. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med. 2013 Nov;19(11):1524-8. [3]. Kim YB, et al. Excitatory GABAergic Action and Increased Vasopressin Synthesis in Hypothalamic Magnocellular Neurosecretory Cells Underlie the High Plasma Level of Vasopressin in Diabetic Rats. Diabetes. 2018 Mar;67(3):486-495.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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