CLP290

SKU: orb1226862

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.

Key Properties

• CAS Number: 1181083-81-7
• MW: 404.46
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₁FN₄O₃S
• SMILES: O=C(N1CCCC1)OC2=CC(F)=CC=C2/C=C(SC(N3CCCCN3)=N4)/C4=O
• Target: Chloride Channel
• Solubility: In Vitro: DMSO : 33.33 mg/mL (82.41 mM)

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CLP-290

Quick Database Links

Gene Symbol

Chloride Channel