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| 10mg |
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Purity: ≥98%
Macitentan (formerly ACT-064992; ACT064992; ACT 064992; Opsumit) is an orally bioavailable and non-peptide, dual antagonist of ETA/ETB endothelin (ET) receptor. The medication has received approval to treat PAH, or pulmonary arterial hypertension. With IC50 values of 0.5 ± 0.2 nM (n = 17), it prevents 125I-ET-1 from binding to recombinant ETA receptors in Chinese hamster ovary cells.
| Targets |
ET-A ( IC50 = 0.5 nM ); ET-B ( IC50 = 0.5 nM )
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| ln Vivo |
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| Animal Protocol |
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| References |
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| Molecular Formula |
C19H20BR2N6O4S
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| Molecular Weight |
588.27
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| Exact Mass |
585.96
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| Elemental Analysis |
C, 38.79; H, 3.43; Br, 27.17; N, 14.29; O, 10.88; S, 5.45
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| CAS # |
441798-33-0
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| Related CAS # |
Macitentan-d4; 1258428-05-5; Macitentan (n-butyl analogue); 556797-16-1
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| Appearance |
Solid powder
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| SMILES |
CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br
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| InChi Key |
JGCMEBMXRHSZKX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27)
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| Chemical Name |
5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-N-(propylsulfamoyl)pyrimidin-4-amine
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| Synonyms |
ACT 064992; Macitentan; ACT-064992; ACT064992; trade name: Opsumit
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04567602 | Active Recruiting |
Drug: PAH medication | Pulmonary Arterial Hypertension | Janssen-Cilag S.p.A. | October 6, 2020 | N/A |
| NCT03904693 | Active Recruiting |
Drug: Placebo macitentan Drug: Placebo FDC Drug: Tadalafil 40 mg Drug: Placebo tadalafil |
Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH) |
Actelion | July 29, 2019 | Phase 3 |
| NCT04271475 | Active Recruiting |
Drug: Macitentan Drug: Placebo |
Chronic Thromboembolic Pulmonary Hypertension |
Actelion | July 7, 2020 | Phase 3 |
| NCT03422328 | Active Recruiting |
Drug: macitentan | Pulmonary Arterial Hypertension Chronic Thromboembolic Pulmonary Hypertension |
Actelion | April 5, 2018 | Phase 3 |
| NCT04780932 | Recruiting | Drug: Placebo Drug: Macitentan 10mg |
Chronic Disease Inoperable Disease |
Assistance Publique - Hôpitaux de Paris |
June 14, 2021 | Phase 2 Phase 3 |
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