CLP290( CLP-290 )

Catalog No. M10617 CAS No. 1181083-81-7

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

CLP290
Note

Research use only, not for human use.
Brief Description

CLP290 (CLP-290) is an orally acirtve small molecule K+-Cl- cotransporter isotype 2 (KCC2) activator, the carbamate prodrug of CLP257.
Description

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.
In Vitro

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In Vivo

CLP290 (oral gavage; 100 mg/kg; twice a day; 7 day) enhances KCC2 activity and restores Cl-?transport in superficial dorsal horn (SDH)neurons of morphine-treated rats, and prevents morphine-induced hyperalgesia (MIH) in rat. Animal Model:Adult male rats (300?g, >postnatal day 60)Dosage:100 mg/kg Administration:Oral gavage; 100 mg/kg; twice a day; 7day Result:Rescued established MIH and prevented its development by restoring Cl-?transport or preventing its deficiency in the SDH.
Synonyms

CLP-290
Pathway

Membrane Transporter/Ion Channel
Target

Chloride Channel
Recptor

Chloride Channel
Research Area

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Indication

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CAS Number

1181083-81-7
Formula Weight

404.46
Molecular Formula

C19H21FN4O3S
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 33.33 mg/mL (82.41 mM)
SMILES

O=C(N1CCCC1)OC2=CC(F)=CC=C2/C=C(SC(N3CCCCN3)=N4)/C4=O
Chemical Name

[5-Fluoro-2-[(Z)-(2-hexahydropyridazin-1-yl-4-oxo-thiazol-5-ylidene)methyl]phenyl] pyrrolidine-1-carboxylate

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.

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