KCC2 blocker 1

Names

[ Name ]:
KCC2 blocker 1

Biological Activity

[Description]:

KCC2 blocker 1 is an orally active and selective K+-Cl- cotransporter KCC2 blocker with an IC50 of 1 μM. KCC2 blocker 1 is a benzyl prolinate and has antiepileptic effect[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

IC50: 1 μM (KCC2)[1]

[In Vitro]

KCC2 blocker 1 (compound 13; 100 μM) inhibits NKCC1 with 35%.

[In Vivo]

KCC2 blocker 1 (compound 13; 1 mg/kg iv and 6 mg/kg po) has a t1/2 of 0.3 hours, a CL of 26 mL/min/kg, a C max of 457 ng/mL and a AUC of 726 ng•h/mL for male Wistar rats[1]. Animal Model: Male Wistar rats[1] Dosage: 1 mg/kg or 6 mg/kg (Pharmacokinetic Analysis) Administration: IV (1 mg/kg) and PO (6 mg/kg) Result: Had a t1/2 of 0.3 hours, a CL of 26 mL/min/kg, a C max of 457 ng/mL and a AUC of 726 ng•h/mL.

[References]

[1]. Pégurier C, et al. Benzyl prolinate derivatives as novel selective KCC2 blockers. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2542-5.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₅NO₅S

[ Molecular Weight ]:
415.50

[ Storage condition ]:
-20°C

KCC2 blocker 1

Names

Biological Activity

Chemical & Physical Properties

Related Compounds