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Aprocitentan (Alias: ACT-132577)

Name: Aprocitentan
Brand: TargetMol
SKU: T7817
Price: 53 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T7817 Copy Product Info

Purity: 99.17%

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Aprocitentan (ACT-132577) is ETA and ETB antagonist .

Aprocitentan

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Catalog No. T7817

Alias ACT-132577

Aprocitentan (ACT-132577) is ETA and ETB antagonist .

Cas No. 1103522-45-7

Pack Size	Price	USA Stock	Global Stock
1 mg	$53	In Stock	In Stock
5 mg	$118	In Stock	In Stock
10 mg	$178	In Stock	In Stock
25 mg	$328	-	In Stock
50 mg	$463	-	In Stock
100 mg	$690	-	In Stock
200 mg	$933	-	In Stock
1 mL x 10 mM (in DMSO)	$145	In Stock	In Stock

In stock · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.17%

Color:White

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COA HNMR LCMS

Product Introduction

Aprocitentan AI Summary

Aprocitentan is a potent ETA receptor antagonist with an IC50 value of 3.4 nM, showing high affinity and selectivity compared to its lower affinity ETB receptor antagonistic activity, evidenced by an IC50 value of 987.0 nM. It also exhibits antiviral activity, as demonstrated by its ability to inhibit SARS-CoV-2 induced cytotoxicity in Caco-2 cells by -1.01% at a concentration of 10 µM after 48 hours of exposure, and shows 0.0% inhibition in VERO-6 cells under similar conditions. Additionally, the compound inhibits the SARS-CoV-2 3CL-Pro protease by 8.054% at 20 µM. Finally, Aprocitentan demonstrates inhibitory activity against the human HDAC6 enzyme, with inhibition percentages of -2.24% and -3.72% in enzymatic assays using commercial and custom peptide substrates, respectively..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Aprocitentan (ACT-132577) is ETA and ETB antagonist .
Targets&IC50	ETB:5.5 (pA2), ETB:987 nM (IC50) , ETA:3.4 nM (IC50) , ETA:6.7 (pA2)
Synonyms	ACT-132577

Chemical Properties

Molecular Weight	546.19
Formula	C₁₆H₁₄Br₂N₆O₄S
Cas No.	1103522-45-7
Smiles	NS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 65 mg/mL (119.01 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.66 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	1.8309 mL	9.1543 mL	18.3086 mL	91.5432 mL
5 mM	0.3662 mL	1.8309 mL	3.6617 mL	18.3086 mL
10 mM	0.1831 mL	0.9154 mL	1.8309 mL	9.1543 mL
20 mM	0.0915 mL	0.4577 mL	0.9154 mL	4.5772 mL
50 mM	0.0366 mL	0.1831 mL	0.3662 mL	1.8309 mL
100 mM	0.0183 mL	0.0915 mL	0.1831 mL	0.9154 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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 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