Shopping Cart

Your shopping cart is currently empty

Macitentan

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

🥰Excellent

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

🥰Excellent

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	USA Warehouse	Global Warehouse
10 mg	$37	In Stock	In Stock
25 mg	$44	In Stock	In Stock
50 mg	$51	In Stock	In Stock
100 mg	$76	In Stock	In Stock
500 mg	$178	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$34	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

Questions

Batch Information

Select Batch

Purity:99.88%

Color:White

Resource Download

COA HNMR LCMS

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

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: 242.5 mg/mL (412.23 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

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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