CLP290

Research use only, not for human use.

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

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.

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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.

CLP-290

Membrane Transporter/Ion Channel

Chloride Channel

Chloride Channel

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1181083-81-7

404.46

C19H21FN4O3S

>98% (HPLC)

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

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

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

(-20℃)

With Ice Pack

≥ 2 years