Cat. No.: HY-14184

Macitentan

(Synonyms: ACT-064992)

14 Cited Publications

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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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Pureté: 99.85%
CAS No.: 441798-33-0
Formule: C₁₉H₂₀Br₂N₆O₄S
Masse moléculaire:588.27

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Macitentan Chemical Structure

CAS No.: 441798-33-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (14)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target

ET_A

ET_B

Voir tous les produits spécifiques à Isoform Endothelin Receptor :

ET_A
ET_B

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.5 nM Compound: 17, Macitentan, ACT-064992	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	[PMID: 22862294]
CHO	IC₅₀	0.5 nM Compound: 43	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	[PMID: 27321813]
CHO	IC₅₀	10 mM Compound: Macitentan	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	[PMID: 31439379]
CHO	IC₅₀	3.4 nM Compound: 43	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	[PMID: 27321813]
CHO	IC₅₀	391 nM Compound: 17, Macitentan, ACT-064992	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]
CHO	IC₅₀	391 nM Compound: 43	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	[PMID: 27321813]
CHO	IC₅₀	987 nM Compound: 43	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	[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.

In Vivo

Macitentan (ACT-064992; 25 mg/kg/day, p.o.) prevents increased production of vasoactive and fibrogenic factors, NF-κB activation, structural and functional changes, and increases extracellular matrix protein production in type 2 diabetes in type 2 diabetes^[2].
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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 441798-33-0
Appearance Solid
Masse moléculaire 588.27
Formule C₁₉H₂₀Br₂N₆O₄S
Color White to off-white
SMILES

BrC1=CN=C(OCCOC2=C(C3=CC=C(Br)C=C3)C(NS(NCCC)(=O)=O)=NC=N2)N=C1
Synonyms

ACT-064992
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

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

The Endothelin Receptor Antagonist Macitentan Inhibits Human Cytomegalovirus Infection. [Abstract]

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

Endothelin-1 induces a strong pressor effect in ball pythons (Python regius). [Abstract]

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
Patent

US20220317132A1.
Patent

US20220242943A1.
JPQA

18 June 2015.

Solvant et solubilité

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6999 mL

8.4995 mL

16.9990 mL

5 mM

0.3400 mL

1.6999 mL

3.3998 mL

10 mM

0.1700 mL

0.8499 mL

1.6999 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocole

Animal Administration^[2]

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.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Macitentan

14 Cited Publications

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Macitentan

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Publications Citing Use of MedChemExpress (MCE) Macitentan

Voir tous les produits spécifiques à Isoform Endothelin Receptor

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Macitentan Related Classifications

Cat. No.: HY-14184