DMP-543
Based on 1 Customer Validation
DMP-543 (XR-543) is a KV7 channel blocker, also acts as a potent neurotransmitter release enhancer.
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- Pureté: 99.96%
- CAS No.: 160588-45-4
- Formule: C26H18F2N2O
- Masse moléculaire:412.43
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Stockage: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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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
KV7 channel
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | CC50 |
77 μM
Compound: 3; DMP-543
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Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 18 hrs by celltiter-glo assay
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 18 hrs by celltiter-glo assay
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[PMID: 31668424] |
| HEK293 | IC50 |
0.048 μM
Compound: 3; DMP-543
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Inhibition of Kv7.2 in human HEK293 cells incubated for 1 hr by thallium flux assay
Inhibition of Kv7.2 in human HEK293 cells incubated for 1 hr by thallium flux assay
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[PMID: 31668424] |
| HEK293 | IC50 |
32 μM
Compound: 3; DMP-543
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Inhibition of ERG in human HEK293 cells incubated for 1 hr by thallium flux assay
Inhibition of ERG in human HEK293 cells incubated for 1 hr by thallium flux assay
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[PMID: 31668424] |
| HepG2 | CC50 |
132 μM
Compound: 3; DMP-543
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 18 hrs by celltiter-glo assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 18 hrs by celltiter-glo assay
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[PMID: 31668424] |
DMP-543 enhances [3H]ACh release from rat brain slices, with an EC50 of 700 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 160588-45-4
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Appearance Solid
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Masse moléculaire 412.43
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Formule C26H18F2N2O
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Color White to yellow
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SMILES
O=C1C2=C(C=CC=C2)C(CC3=CC(F)=NC=C3)(CC4=CC(F)=NC=C4)C5=CC=CC=C15
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Synonyms
XR-543
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (242.47 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.06 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 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 (6.06 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.
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 (280 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]. Ipavec V, et al. KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus. Pharmacol Res. 2011 Oct;64(4):397-409. [Content Brief]
[2]. Zaczek R, et al. Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine. J Pharmacol Exp Ther. 1998 May;285(2):724-30. [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 | 2.4247 mL | 12.1233 mL | 24.2465 mL | 60.6163 mL |
| 5 mM | 0.4849 mL | 2.4247 mL | 4.8493 mL | 12.1233 mL | |
| 10 mM | 0.2425 mL | 1.2123 mL | 2.4247 mL | 6.0616 mL | |
| 15 mM | 0.1616 mL | 0.8082 mL | 1.6164 mL | 4.0411 mL | |
| 20 mM | 0.1212 mL | 0.6062 mL | 1.2123 mL | 3.0308 mL | |
| 25 mM | 0.0970 mL | 0.4849 mL | 0.9699 mL | 2.4247 mL | |
| 30 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0205 mL | |
| 40 mM | 0.0606 mL | 0.3031 mL | 0.6062 mL | 1.5154 mL | |
| 50 mM | 0.0485 mL | 0.2425 mL | 0.4849 mL | 1.2123 mL | |
| 60 mM | 0.0404 mL | 0.2021 mL | 0.4041 mL | 1.0103 mL | |
| 80 mM | 0.0303 mL | 0.1515 mL | 0.3031 mL | 0.7577 mL | |
| 100 mM | 0.0242 mL | 0.1212 mL | 0.2425 mL | 0.6062 mL |
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