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).
For research use only. We do not sell to patients.
- Purity : 99.85%
- CAS No.: 441798-33-0
- Formula: C19H20Br2N6O4S
- Molecular Weight:588.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
- Protocols
- Purity & Documentation
- References
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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 Sep: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.
Customer Validation & Images
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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WB
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WB
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In Vivo Efficacy Study
Biological Activity
Description
IC50 & Target
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ETA |
ETB |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 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] |
In Vitro
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. Further protocols information, click here.
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 441798-33-0
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Appearance Solid
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Molecular Weight 588.27
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Formula 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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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
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
Macitentan purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2024 Jul;13(7):e12479. [Abstract]
Growth curves of EMT6 (top), levels of plasma sEV PD-L1 (middle), and plasma sEV concentrations (bottom) of immunocompetent mice subjected to the indicated treatments (n = 5−6). Vertical dotted lines represent the beginning of macitentan (MAC, 50 mg/kg, oral) administration.
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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
Macitentan purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Jan 31;12(5):1971-1987. [Abstract]
The amounts of protein in the EVs derived from MDA-MB231 and 4T1 cells in the absence or presence of MAC (Macitentan).
Macitentan purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Jan 31;12(5):1971-1987. [Abstract]
The immunoblot of various proteins in EV and whole-cell lysates from MDA-MB231 and 4T1 cells with or without MAC (Macitentan).
Macitentan purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Jan 31;12(5):1971-1987. [Abstract]
The immunoblot of PD-L1 and CD63 in the EVs from MDA-MB231 and 4T1 cells treated with or without MAC (Macitentan) at the indicated concentration (top). The densitometric analysis of the relative intensity of the protein bands (bottom) (n = 3).
Macitentan purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Jan 31;12(5):1971-1987. [Abstract]
We studied whether the antitumor immunity boosted by the combination therapy could be reversed by injecting exogenous EV PD-L1. We injected EMT6 tumor-derived EVs intravenously into EMT6 tumor-bearing mice co-treated with MAC (Macitentan) and the anti-PD-L1 antibody.
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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 Sep: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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Solvent & Solubility
In Vitro:
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)
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 (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.
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.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Purity & Documentation
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Data Sheet (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)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
References
[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 |
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| 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 |
Macitentan Related Classifications
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