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Macitentan

Name: Macitentan
Brand: TargetMol
SKU: T2561
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.88%

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
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:99.88%

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COA LCMS HNMR

Product Introduction

Bioactivity

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.
Synonyms	ACT-064992

Chemical Properties

Molecular Weight	588.27
Formula	C₁₉H₂₀Br₂N₆O₄S
Cas No.	441798-33-0
Smiles	N(S(NCCC)(=O)=O)C=1C(=C(OCCOC=2N=CC(Br)=CN2)N=CN1)C3=CC=C(Br)C=C3
Relative Density.	1.675 g/cm3
Color	White
Appearance	Solid

Storage & Solubility Information

Storage

store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (158.09 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.61 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6999 mL	8.4995 mL	16.9990 mL	84.9950 mL
5 mM	0.3400 mL	1.6999 mL	3.3998 mL	16.9990 mL
10 mM	0.1700 mL	0.8499 mL	1.6999 mL	8.4995 mL
20 mM	0.0850 mL	0.4250 mL	0.8499 mL	4.2497 mL
50 mM	0.0340 mL	0.1700 mL	0.3400 mL	1.6999 mL
100 mM	0.0170 mL	0.0850 mL	0.1700 mL	0.8499 mL

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In Vivo Formulation Calculator (Clear solution)

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:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(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 TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc