1. Membrane Transporter/Ion Channel
  2. Potassium Channel

VU0463271 (Synonyms: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide)

Cat. No.: HY-110110
Handling Instructions

VU0463271 is a potent KCC2 antagonist, with an IC50 of 61 nM.

For research use only. We do not sell to patients.

VU0463271 Chemical Structure

VU0463271 Chemical Structure

CAS No. : 1391737-01-1

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

VU0463271 is a potent KCC2 antagonist, with an IC50 of 61 nM.

IC50 & Target

IC50: 61 nM (KCC2)[1].

In Vitro

VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels and transporters. It is also found rapidly cleared in vitro[1].

In Vivo

VU0463271 is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg) following intravenous administration (1 mg/kg); the low volume of distribution at steady state (Vss 0.4 L/kg), coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6144 mL 13.0719 mL 26.1438 mL
5 mM 0.5229 mL 2.6144 mL 5.2288 mL
10 mM 0.2614 mL 1.3072 mL 2.6144 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

382.50

Formula

C₁₉H₁₈N₄OS₂

CAS No.

1391737-01-1

SMILES

O=C(N(C1CC1)C2=NC(C)=CS2)CSC3=NN=C(C4=CC=CC=C4)C=C3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
VU0463271
Cat. No.:
HY-110110
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VU0463271

Cat. No.: HY-110110