PD-118057
Based on 1 Customer Validation
PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability.
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- Pureté: 98.06%
- CAS No.: 313674-97-4
- Formule: C21H17Cl2NO2
- Masse moléculaire:386.27
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Human ether-a-go-go-related gene channel[1]
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.
Chemical Information
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CAS No. 313674-97-4
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Appearance Solid
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Masse moléculaire 386.27
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Formule C21H17Cl2NO2
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Color Off-white to light yellow
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SMILES
O=C(O)C1=CC=CC=C1NC2=CC=C(CCC3=CC=C(Cl)C(Cl)=C3)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Mao H, et al. Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. PLoS One. 2013 Jun 19;8(6):e65481. [Content Brief]
[2]. Yeung SY, et al. Pharmacological and biophysical isolation of K+ currents encoded by ether-à-go-go-related genes in murine hepatic portal vein smooth muscle cells. Am J Physiol Cell Physiol. 2007 Jan;292(1):C468-76. [Content Brief]
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 |
PD-118057 Related Classifications
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