Macitentan
Based on 14 publication(s) in Google Scholar
Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
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- Pureza: 99.85%
- No. CAS: 441798-33-0
- Fòrmula: C19H20Br2N6O4S
- Peso molecular:588.27
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Macitentan
More- J Extracell Vesicles. 2024 Jul;13(7):e12479. [Abstract]
- Theranostics. 2022 Jan 31;12(5):1971-1987. [Abstract]
- Biosens Bioelectron. 2025 Jan 1:267:116863. [Abstract]
- Biomater Res. 2025 Jun 9:29:0214. [Abstract]
- Cancer Cell Int. 2023 Dec 10;23(1):318. [Abstract]
- Biochem Pharmacol. 2025 Jun 9:239:117019. [Abstract]
- Cells. 2021 Nov 8;10(11):3072. [Abstract]
- BMC Cancer. 2018 Feb 6;18(1):154. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Feb 1:1252:124443. [Abstract]
- Comp Biochem Physiol A Mol Integr Physiol. 2020 Mar;241:110620. [Abstract]
- bioRxiv. 2024 Jun 1:2024.05.27.596052. [Abstract]
- Patent. US20220317132A1.
- Patent. US20220242943A1.
- JPQA. 18 June 2015.
Actividad biológica
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ETA |
ETB |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.5 nM
Compound: 17, Macitentan, ACT-064992
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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 |
0.5 nM
Compound: 43
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Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
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[PMID: 27321813] |
| CHO | IC50 |
10 mM
Compound: Macitentan
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Inhibition of human recombinant NTCP expressed in CHO cells assessed as reduction in [3H]taurocholate uptake preincubated for 1 hr by radioactive scintillation counting method
Inhibition of human recombinant NTCP expressed in CHO cells assessed as reduction in [3H]taurocholate uptake preincubated for 1 hr by radioactive scintillation counting method
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[PMID: 31439379] |
| CHO | IC50 |
3.4 nM
Compound: 43
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Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1
Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1
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[PMID: 27321813] |
| CHO | IC50 |
391 nM
Compound: 17, Macitentan, ACT-064992
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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
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[PMID: 22862294] |
| CHO | IC50 |
391 nM
Compound: 43
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Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
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[PMID: 27321813] |
| CHO | IC50 |
987 nM
Compound: 43
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Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
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[PMID: 27321813] |
Tube formation ability is restored when microvascular endothelial cells are preincubated with BOS or macitentan (ACT-064992), also reducing the expression of mesenchymal markers and restoring CD31 expression and the imbalance between VEGF-A and VEGF-A165b[1].
Macitentan inhibits OATP1B1-mediated uptake of atorvastatin and OATP1B3-mediated uptake of estrone-3-sulfate with IC50 ± SE values of 6.3 ± 0.7 and 11.8 ± 5.0 μM, respectively[3].
Treatment with macitentan or with ACT-132577 does not lead to intracellular accumulation of R123 in HeyA8-MDR, showing that these compounds are not P-gp inhibitors[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Macitentan (10 mg/kg, p.o.) coupled with once-per-week 5 mg/kg taxol, significantly reduces the weight (size) of HeyA8-MDR tumors in mice. Combination therapy with macitentan (10 or 50 mg/kg, but not 5 mg/kg) and taxol or macitentan (10 mg/kg) and cisplatinum significantly reduces the number of proliferating Ki-67-positive cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 441798-33-0
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Appearance Solid
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Peso molecular 588.27
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Fòrmula C19H20Br2N6O4S
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Color White to off-white
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SMILES
BrC1=CN=C(OCCOC2=C(C3=CC=C(Br)C=C3)C(NS(NCCC)(=O)=O)=NC=N2)N=C1
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Synonyms
ACT-064992
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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J Extracell Vesicles
Extracellular vesicle isolation and counting system (EVics) based on simultaneous tandem tangential flow filtration and large field-of-view light scattering. [Abstract]2024 Jul;13(7):e12479. PMID: 38978321 -
Theranostics
Macitentan improves antitumor immune responses by inhibiting the secretion of tumor-derived extracellular vesicle PD-L1. [Abstract]2022 Jan 31;12(5):1971-1987. PMID: 35265193 -
Biosens Bioelectron
High-precision extracellular-vesicle isolation-analysis integrated platform for rapid cancer diagnosis directly from blood plasma. [Abstract]2025 Jan 1:267:116863. PMID: 39442437 -
Biomater Res
Dual-Active Nanoimmunomodulators for the Synergistic Enhancement of the Antitumor Efficacy of Photodynamic Immunotherapy. [Abstract]2025 Jun 9:29:0214. PMID: 40491506 -
Cancer Cell Int
Targeting the Endothelin-1 pathway to reduce invasion and chemoresistance in gallbladder cancer cells. [Abstract]2023 Dec 10;23(1):318. PMID: 38072958 -
Biochem Pharmacol
An updated review on the inhibition of exosome biogenesis, release, and uptake: a potential anticancer approach. [Abstract]2025 Jun 9:239:117019. PMID: 40499840 -
Cells
2021 Nov 8;10(11):3072. PMID: 34831300 -
BMC Cancer
Overexpression of endothelin B receptor in glioblastoma: a prognostic marker and therapeutic target?. [Abstract]2018 Feb 6;18(1):154. PMID: 29409474 -
J Chromatogr B Analyt Technol Biomed Life Sci
A simple HPLC-UV method for monitoring therapeutic adherence in pulmonary arterial hypertension. [Abstract]2025 Feb 1:1252:124443. PMID: 39787725 -
Comp Biochem Physiol A Mol Integr Physiol
2020 Mar;241:110620. PMID: 31770594 -
bioRxiv
Exploring Integrin α5β1 as a Potential Therapeutic Target for Pulmonary Arterial Hypertension: Insights from Comprehensive Multicenter Preclinical Studies. [Abstract]2024 Jun 1:2024.05.27.596052. PMID: 38854025 -
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Solvente y solubilidad
DMSO : ≥ 50 mg/mL (84.99 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.25 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.
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.
Protocolo
Male db/db mice and age and sex-matched controls (27-32 g) are used for the assay. RandomLy selected diabetic animals are monitored for either 2 months or for 4 months after onset of diabetes. Groups (n=7/group) of the diabetic mice are subjected to oral macitentan treatment for the same period (25 mg/kg/day, food admix). The animals are monitored through assessment of body weight and blood glucose.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Portuguese - PT (418 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Corallo C, et al. Bosentan and macitentan prevent the endothelial-to-mesenchymal transition (EndoMT) in systemic sclerosis: in vitro study. Arthritis Res Ther. 2016 Oct 6;18(1):228. [Content Brief]
[2]. Sen S, et al. Renal, retinal and cardiac changes in type 2 diabetes are attenuated by macitentan, a dual endothelin receptor antagonist. Life Sci. 2012 Apr 13. [Content Brief]
[3]. Bruderer S, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J. 2012 Mar;14(1):68-78. [Content Brief]
[4]. Kim SJ, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol. 2012 Feb;5(1):39-47. [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, 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 | 1.6999 mL | 8.4995 mL | 16.9990 mL | 42.4975 mL |
| 5 mM | 0.3400 mL | 1.6999 mL | 3.3998 mL | 8.4995 mL | |
| 10 mM | 0.1700 mL | 0.8499 mL | 1.6999 mL | 4.2497 mL | |
| 15 mM | 0.1133 mL | 0.5666 mL | 1.1333 mL | 2.8332 mL | |
| 20 mM | 0.0850 mL | 0.4250 mL | 0.8499 mL | 2.1249 mL | |
| 25 mM | 0.0680 mL | 0.3400 mL | 0.6800 mL | 1.6999 mL | |
| 30 mM | 0.0567 mL | 0.2833 mL | 0.5666 mL | 1.4166 mL | |
| 40 mM | 0.0425 mL | 0.2125 mL | 0.4250 mL | 1.0624 mL | |
| 50 mM | 0.0340 mL | 0.1700 mL | 0.3400 mL | 0.8499 mL | |
| 60 mM | 0.0283 mL | 0.1417 mL | 0.2833 mL | 0.7083 mL | |
| 80 mM | 0.0212 mL | 0.1062 mL | 0.2125 mL | 0.5312 mL |
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