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CLP-290

Names

[ CAS No. ]:
1181083-81-7

[ Name ]:
CLP-290

[Synonym ]:
MFCD28166314
1-Pyrrolidinecarboxylic acid, 5-fluoro-2-[(Z)-[4-oxo-2-(tetrahydro-1(2H)-pyridazinyl)-5(4H)-thiazolylidene]methyl]phenyl ester
5-Fluoro-2-{(Z)-[4-oxo-2-(tetrahydro-1(2H)-pyridazinyl)-1,3-thiazol-5(4H)-ylidene]methyl}phenyl 1-pyrrolidinecarboxylate

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
553.7±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C19H21FN4O3S

[ Molecular Weight ]:
404.458

[ Flash Point ]:
288.6±32.9 °C

[ Exact Mass ]:
404.131836

[ LogP ]:
2.89

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.691

Related Compounds