1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. VU0810464

VU0810464 

Cat. No.: HY-127106 Purity: 99.72%
Handling Instructions

VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration.

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

VU0810464 Chemical Structure

VU0810464 Chemical Structure

CAS No. : 2126040-21-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration[1][2].

IC50 & Target

EC50: 165 nM (GIRK 1/2); 720 nM (GIRK1/4 )[1][2]

In Vitro

VU0810464 (0, 0.1, 0.3, 1, 3, 10, 30 μM) produces a concentration‐dependent response curves of currents in SAN and HPC cells, in addition, VU0810464 is 9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells[2].

In Vivo

VU0810464 (intraperitoneal injection; 30 mg/kg, 10 mg/kg; 30mg/kg; pre-treated 30 mins) produces a dose-dependent reduction of SIH response in Male C57BL/6J mice. To test if VU0810464 plays it role through Kir3 channel activation, VU0810464 (10 mg/kg) suppresses the SIH response in wild‐ type mice, but has no impact on Kcnj3−/− mice[2].
VU0810464 (intraperitoneal injection ; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (Kp,uu = 0.83), has a improvement over ML297 (Kp,uu= 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study[2].

Animal Model: Male C57BL/6J mice, Kcnj3−/− siblings female and male C57BL/6J mice
Dosage: 10 mg/kg; 30mg/kg
Administration: Intraperitoneal injection
Result: Reduced stress‐induced hyperthermia (SIH), a physiological test of anxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) −/− mice.
Molecular Weight

349.83

Formula

C₁₈H₂₁ClFN₃O

CAS No.

2126040-21-7

SMILES

O=C(NC1=CC(C)=NN1C2CCCCC2)CC3=CC=C(F)C(Cl)=C3

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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (714.63 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8585 mL 14.2927 mL 28.5853 mL
5 mM 0.5717 mL 2.8585 mL 5.7171 mL
10 mM 0.2859 mL 1.4293 mL 2.8585 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

VU0810464VU 0810464VU-0810464Potassium ChannelKcsAneuronal GIRKHPCSANcellsInhibitorinhibitorinhibit

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VU0810464
Cat. No.:
HY-127106
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