L-706000 free base
Based on 1 Customer Validation
L-706000 (MK 499) free base is a potent hERG channel blocker with an IC50 of 32 nM. L-706000 free base is a class III antiarrhythmic agent that can be used for the study of malignant ventricular tachyarrhythmias.
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 161799-18-4
- Formula: C25H29N3O4S
- Molecular Weight:467.58
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Storage:Powder -20°C, 3 years , 4°C, 2 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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
IC50: 32 nM (hERG channel)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.67 μM
Compound: MK-499
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Displacement of [35S]MK499 from human ERG expressed in HEK293 cells
Displacement of [35S]MK499 from human ERG expressed in HEK293 cells
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[PMID: 20423086] |
Chemical Information
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CAS No. 161799-18-4
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Appearance Solid
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Molecular Weight 467.58
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Formula C25H29N3O4S
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Color Off-white to pink
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SMILES
O[C@@H]1CC2(CCN([C@@](CCC3=C4)([H])CC3=CC=C4C#N)CC2)OC(C1=C5)=CC=C5N[S](C)(=O)=O
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Synonyms
MK 499 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 : 100 mg/mL (213.87 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.35 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.35 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 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:
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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.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. J S Mitcheson, et al. Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate. J Gen Physiol. 2000 Mar;115(3):229-40. [Content Brief]
[2]. S Vickers, et al. Metabolism of MK-499, a class III antiarrhythmic agent, in rats and dogs. Drug Metab Dispos. 1998 May;26(5):388-95. [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 | 2.1387 mL | 10.6934 mL | 21.3867 mL | 53.4668 mL |
| 5 mM | 0.4277 mL | 2.1387 mL | 4.2773 mL | 10.6934 mL | |
| 10 mM | 0.2139 mL | 1.0693 mL | 2.1387 mL | 5.3467 mL | |
| 15 mM | 0.1426 mL | 0.7129 mL | 1.4258 mL | 3.5645 mL | |
| 20 mM | 0.1069 mL | 0.5347 mL | 1.0693 mL | 2.6733 mL | |
| 25 mM | 0.0855 mL | 0.4277 mL | 0.8555 mL | 2.1387 mL | |
| 30 mM | 0.0713 mL | 0.3564 mL | 0.7129 mL | 1.7822 mL | |
| 40 mM | 0.0535 mL | 0.2673 mL | 0.5347 mL | 1.3367 mL | |
| 50 mM | 0.0428 mL | 0.2139 mL | 0.4277 mL | 1.0693 mL | |
| 60 mM | 0.0356 mL | 0.1782 mL | 0.3564 mL | 0.8911 mL | |
| 80 mM | 0.0267 mL | 0.1337 mL | 0.2673 mL | 0.6683 mL | |
| 100 mM | 0.0214 mL | 0.1069 mL | 0.2139 mL | 0.5347 mL |
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