1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. VU0463271 quarterhydrate

VU0463271 quarterhydrate 

Cat. No.: HY-110110A Purity: >98.0%
Handling Instructions

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

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

VU0463271 quarterhydrate Chemical Structure

VU0463271 quarterhydrate Chemical Structure

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1 mg USD 250 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of VU0463271 quarterhydrate:

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Description

VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC50 of 61 nM[1].

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].
VU0463271 is applied to the transected CNS preparation and resulted in a significant increase in firing rates of the Drosophila CNS with 1 μM VU0463271 resulting in a peak firing rate that was a 2.7- and 2.5-fold increase over baseline firing rate for OR and rdl strains, respectively[2].
VU0463271 (10-100 nM) results in approximately 20% reduction of CNS firing frequency within a small percentage of preparations[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

387.00

Formula

C₁₉H₁₈N₄OS₂.₁/₄H₂O

SMILES

O=C(N(C1CC1)C2=NC(C)=CS2)CSC3=NN=C(C4=CC=CC=C4)C=C3.[1/4].O

Shipping

Room temperature in continental US; may vary elsewhere.

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

Purity: >98.0%

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Keywords:

VU0463271 quarterhydratePotassium ChannelKcsAInhibitorinhibitorinhibit

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