2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. PD-118057

PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability.

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

PD-118057 Chemical Structure

PD-118057 Chemical Structure

CAS No. : 313674-97-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 286 In-stock
Solution
10 mM * 1 mL in DMSO USD 286 In-stock
Solid
1 mg USD 120 In-stock
5 mg USD 260 In-stock
10 mg USD 400 In-stock
25 mg USD 760 In-stock
50 mg USD 1200 In-stock
100 mg USD 1920 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

PD-118057 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability[1][2].

IC50 & Target

Human ether-a-go-go-related gene channel[1]
In Vitro

PD-118057 (3 μM and 10 μM) specifically increases hERG current and inhibits action potential duration in guinea pig ventricular muscle in acute isolation of guinea pig cardiomyocytes[2][3].
PD-118057 (10 μM) reverses the current inhibition induced by Dof and Mox without changing the "hump" shape of IKr current recorded by action potential clamp, and only slightly increases the peak value of the suppressed current[3].

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

PD-118057 Related Antibodies
Molecular Weight

386.27

Formula

C21H17Cl2NO2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)C1=CC=CC=C1NC2=CC=C(CCC3=CC=C(Cl)C(Cl)=C3)C=C2
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 (258.89 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 2.5889 mL 12.9443 mL 25.8886 mL
5 mM 0.5178 mL 2.5889 mL 5.1777 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)

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.47 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

Purity: ≥99.0%

COA (247 KB) Elemental Analysis Report (105 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, 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 2.5889 mL 12.9443 mL 25.8886 mL 64.7216 mL
5 mM 0.5178 mL 2.5889 mL 5.1777 mL 12.9443 mL
10 mM 0.2589 mL 1.2944 mL 2.5889 mL 6.4722 mL
15 mM 0.1726 mL 0.8630 mL 1.7259 mL 4.3148 mL
20 mM 0.1294 mL 0.6472 mL 1.2944 mL 3.2361 mL
25 mM 0.1036 mL 0.5178 mL 1.0355 mL 2.5889 mL
30 mM 0.0863 mL 0.4315 mL 0.8630 mL 2.1574 mL
40 mM 0.0647 mL 0.3236 mL 0.6472 mL 1.6180 mL
50 mM 0.0518 mL 0.2589 mL 0.5178 mL 1.2944 mL
60 mM 0.0431 mL 0.2157 mL 0.4315 mL 1.0787 mL
80 mM 0.0324 mL 0.1618 mL 0.3236 mL 0.8090 mL
100 mM 0.0259 mL 0.1294 mL 0.2589 mL 0.6472 mL
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PD-118057 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:

PD-118057313674-97-4PD118057PD 118057Potassium ChannelKcsAmembrane excitabilitymPV smooth muscle cellsDofMoxguinea pig ventricular muscleguinea pig cardiomyocytesInhibitorinhibitorinhibit

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