KCC2 blocker 1

Modify Date: 2024-01-16 17:36:05

KCC2 blocker 1 Structure
KCC2 blocker 1 structure
Common Name KCC2 blocker 1
CAS Number 1228439-36-8 Molecular Weight 415.50
Density N/A Boiling Point N/A
Molecular Formula C22H25NO5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of KCC2 blocker 1


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].

 Names

Name KCC2 blocker 1

 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
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