1228439-36-8

1228439-36-8 structure

Name: KCC2 blocker 1
Chemical Name: KCC2 blocker 1
CAS Number: 1228439-36-8
Molecular Formula: C₂₂H₂₅NO₅S
Molecular Weight: 415.50
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
Create Date: 2020-06-01 10:53:09
Modify Date: 2024-01-16 17:36:05
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].

Name	KCC2 blocker 1

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.