1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. VU 0240551

VU 0240551 

Cat. No.: HY-16689 Purity: 99.56%
Handling Instructions

VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission.

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

VU 0240551 Chemical Structure

VU 0240551 Chemical Structure

CAS No. : 893990-34-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 125 In-stock
Estimated Time of Arrival: December 31
5 mg USD 114 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Description

VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission[1][2].

In Vitro

VU 0240551 reduces the P cell response to GABA in a concentration-dependent manner with 75 and 100 μM treatments causing a significant reduction in GABA-elicited hyperpolarization while 25 μM had no significant effect[2].

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

In Vivo

VU 0240551 (10 μM) significantly blocks the chloride influx in cells from Eu rats but did not affect cells from SL rats[3].

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

Molecular Weight

342.44

Formula

C₁₆H₁₄N₄OS₂

CAS No.
SMILES

O=C(CSC1=NN=C(C2=CC=CC=C2)C=C1)NC3=NC(C)=CS3

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 : ≥ 50 mg/mL (146.01 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9202 mL 14.6011 mL 29.2022 mL
5 mM 0.5840 mL 2.9202 mL 5.8404 mL
10 mM 0.2920 mL 1.4601 mL 2.9202 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: ≥ 2.5 mg/mL (7.30 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.30 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution

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

VU 0240551VU0240551VU-0240551Potassium ChannelKcsAhyperpolarizationPcellstransmissionnon-nociceptiveafferentInhibitorinhibitorinhibit

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Product Name:
VU 0240551
Cat. No.:
HY-16689
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