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Macitentan
Catalog No. T2561Cas No. 441798-33-0
Alias ACT-064992
Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH).
Macitentan
Catalog No. T2561Alias ACT-064992Cas No. 441798-33-0
Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 10 mg | $37 | In Stock | |
| 25 mg | $44 | In Stock | |
| 50 mg | $51 | In Stock | |
| 100 mg | $76 | In Stock | |
| 500 mg | $178 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $34 | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH). |
| Targets&IC50 | ETB:391 nM, ETA:0.5 nM |
| In vitro | In DOCA-salt-induced hypertensive rats, Macitentan (10 mg/kg) demonstrated a dose-dependent reduction in mean arterial blood pressure. Similarly, in a model of pulmonary arterial hypertension using monocrotaline-treated rats, oral administration of Macitentan (30 mg/kg/day) dose-dependently prevented the development of pulmonary arterial hypertension and right ventricular hypertrophy. Additionally, in type 2 diabetic db/db mice, oral Macitentan (25 mg/kg/day) reduced mRNA expression while concurrently enhancing NF-κB activation. |
| In vivo | In primary human lung smooth muscle cells (IC50=1 nM), Macitentan inhibits the increase of intracellular calcium ions induced by ET-1. Additionally, Macitentan suppresses ET-1-induced contraction in isolated rat aortic rings. Furthermore, in isolated rat tracheal rings, Macitentan inhibits contraction induced by S6c. |
| Alias | ACT-064992 |
| Molecular Weight | 588.27 |
| Formula | C19H20Br2N6O4S |
| Cas No. | 441798-33-0 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 93 mg/mL (158.1 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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