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

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.

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VU 0240551 Chemical Structure

VU 0240551 Chemical Structure

CAS No. : 893990-34-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 96 In-stock
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10 mM * 1 mL in DMSO USD 96 In-stock
Solid
5 mg USD 88 In-stock
10 mg USD 156 In-stock
25 mg USD 329 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

VU 0240551 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE VU 0240551

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 50 μM
Compound: 1, VU0240511
Antagonist activity at NKKC1 expressed in human HEK293 cells assessed as [86Rb] uptake after 30 mins by scintillation counting
Antagonist activity at NKKC1 expressed in human HEK293 cells assessed as [86Rb] uptake after 30 mins by scintillation counting
[PMID: 22727639]
HEK293 IC50
568 nM
Compound: 1, VU0240511
Antagonist activity at KCC2 expressed in human HEK293 cells assessed as decrease in Tl-stimulated fluorescence increase after 8 mins by fluorescence analysis
Antagonist activity at KCC2 expressed in human HEK293 cells assessed as decrease in Tl-stimulated fluorescence increase after 8 mins by fluorescence analysis
[PMID: 22727639]
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].

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

VU 0240551 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

342.44

Formula

C16H14N4OS2
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (146.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.97%

SDS (393 KB)

COA (246 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9202 mL 14.6011 mL 29.2022 mL 73.0055 mL
5 mM 0.5840 mL 2.9202 mL 5.8404 mL 14.6011 mL
10 mM 0.2920 mL 1.4601 mL 2.9202 mL 7.3005 mL
15 mM 0.1947 mL 0.9734 mL 1.9468 mL 4.8670 mL
20 mM 0.1460 mL 0.7301 mL 1.4601 mL 3.6503 mL
25 mM 0.1168 mL 0.5840 mL 1.1681 mL 2.9202 mL
30 mM 0.0973 mL 0.4867 mL 0.9734 mL 2.4335 mL
40 mM 0.0730 mL 0.3650 mL 0.7301 mL 1.8251 mL
50 mM 0.0584 mL 0.2920 mL 0.5840 mL 1.4601 mL
60 mM 0.0487 mL 0.2434 mL 0.4867 mL 1.2168 mL
80 mM 0.0365 mL 0.1825 mL 0.3650 mL 0.9126 mL
100 mM 0.0292 mL 0.1460 mL 0.2920 mL 0.7301 mL
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VU 0240551 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU 0240551893990-34-6VU0240551VU-0240551Potassium ChannelKcsAhyperpolarizationPcellstransmissionnon-nociceptiveafferentInhibitorinhibitorinhibit

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