1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. VU0542270

VU0542270 is a selective vascular Kir6.1/SUR2B KATP channel inhibitor with an IC50 value of 100 nM. VU0542270 has an IC50 > 30 μM for the other nine members of the Kir channel family. VU0542270 can be used in the study of cardiovascular disease.

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

VU0542270 Chemical Structure

VU0542270 Chemical Structure

CAS No. : 1396814-79-1

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Based on 1 publication(s) in Google Scholar

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Description

VU0542270 is a selective vascular Kir6.1/SUR2B KATP channel inhibitor with an IC50 value of 100 nM. VU0542270 has an IC50 > 30 μM for the other nine members of the Kir channel family. VU0542270 can be used in the study of cardiovascular disease[1].

In Vitro

VU0542270 (0-10 μM; 0-90 min) has an inhibitory effect on Kir6.1/SUR2B and can completely inhibit KATP current[1].
VU0542270 (1 nM-100 μM; 20 min) induces contraction of isolated ductus arteriosus in pregnant mice, similar to Glibenclamide (HY-15206)[1].

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

In Vivo

Pharmacokinetic Analysis in rats[1]

Route Dose (mg/kg) CLp (mL/min per kg) t1/2 (h) MRT (h) VSS (L/kg)
i.v. 1 17.7 0.64 0.19 0.20

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

Molecular Weight

335.47

Formula

C14H13N3OS3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(CNC(NC2=CC=CS2)=O)SC(C3=CC=CS3)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (298.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9809 mL 14.9045 mL 29.8089 mL
5 mM 0.5962 mL 2.9809 mL 5.9618 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9809 mL 14.9045 mL 29.8089 mL 74.5223 mL
5 mM 0.5962 mL 2.9809 mL 5.9618 mL 14.9045 mL
10 mM 0.2981 mL 1.4904 mL 2.9809 mL 7.4522 mL
15 mM 0.1987 mL 0.9936 mL 1.9873 mL 4.9682 mL
20 mM 0.1490 mL 0.7452 mL 1.4904 mL 3.7261 mL
25 mM 0.1192 mL 0.5962 mL 1.1924 mL 2.9809 mL
30 mM 0.0994 mL 0.4968 mL 0.9936 mL 2.4841 mL
40 mM 0.0745 mL 0.3726 mL 0.7452 mL 1.8631 mL
50 mM 0.0596 mL 0.2981 mL 0.5962 mL 1.4904 mL
60 mM 0.0497 mL 0.2484 mL 0.4968 mL 1.2420 mL
80 mM 0.0373 mL 0.1863 mL 0.3726 mL 0.9315 mL
100 mM 0.0298 mL 0.1490 mL 0.2981 mL 0.7452 mL
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  • 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.

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Product Name:
VU0542270
Cat. No.:
HY-162322
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