Macitentan n-butyl analogue
Based on 1 Customer Validation
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
For research use only. We do not sell to patients.
- Purity: 99.35%
- CAS No.: 556797-16-1
- Formula: C20H21Br2N5O4S
- Molecular Weight:587.28
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.1 nM
Compound: 70
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Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
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[PMID: 22862294] |
| CHO | IC50 |
2424 nM
Compound: 70
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Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
|
[PMID: 22862294] |
Chemical Information
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CAS No. 556797-16-1
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Appearance Solid
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Molecular Weight 587.28
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Formula C20H21Br2N5O4S
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Color White to yellow
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SMILES
BrC1=CN=C(OCCOC2=C(C3=CC=C(Br)C=C3)C(NS(CCCC)(=O)=O)=NC=N2)N=C1
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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 2 years -20°C 1 year
Solvent & Solubility
DMSO : 125 mg/mL (212.85 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Purity & Documentation
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Data Sheet (243 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7028 mL | 8.5138 mL | 17.0277 mL | 42.5691 mL |
| 5 mM | 0.3406 mL | 1.7028 mL | 3.4055 mL | 8.5138 mL | |
| 10 mM | 0.1703 mL | 0.8514 mL | 1.7028 mL | 4.2569 mL | |
| 15 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8379 mL | |
| 20 mM | 0.0851 mL | 0.4257 mL | 0.8514 mL | 2.1285 mL | |
| 25 mM | 0.0681 mL | 0.3406 mL | 0.6811 mL | 1.7028 mL | |
| 30 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4190 mL | |
| 40 mM | 0.0426 mL | 0.2128 mL | 0.4257 mL | 1.0642 mL | |
| 50 mM | 0.0341 mL | 0.1703 mL | 0.3406 mL | 0.8514 mL | |
| 60 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL | |
| 80 mM | 0.0213 mL | 0.1064 mL | 0.2128 mL | 0.5321 mL | |
| 100 mM | 0.0170 mL | 0.0851 mL | 0.1703 mL | 0.4257 mL |