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Avosentan

Name: Avosentan
Brand: TargetMol
SKU: TQ0282
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0282Cas No. 290815-26-8

Alias SPP-301, Ro 67-0565

Avosentan(Ro 67-0565; SPP-301) is a potent endothelin receptor (ETA) antagonist with strong inhibitory effects on endothelin-1-induced contraction and may have protective effects against chronic kidney disease. [2]

Avosentan

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Purity: 99.47%

Catalog No. TQ0282Alias SPP-301, Ro 67-0565Cas No. 290815-26-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	-	In Stock
5 mg	$77	-	In Stock
10 mg	$108	-	In Stock
25 mg	$228	-	In Stock
50 mg	$396	-	In Stock
100 mg	$579	4-6 weeks	4-6 weeks
1 mL x 10 mM (in DMSO)	$81	-	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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.

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Batch Information

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Purity:99.47%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HPLC HNMR

Product Introduction

Avosentan AI Summary

Avosentan exhibits multiple bioactivities with notable antiviral and receptor antagonistic effects. It shows antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity of both Caco-2 and VERO-6 cells at a 10 µM concentration after 48 hours, with inhibition rates of -7.75% and 0.03%, respectively. In enzymatic assays, it inhibits the SARS-CoV-2 3CL-Pro protease by 20.61% at a 20 µM concentration. Additionally, it acts as an antagonist at ET receptors, demonstrating strong binding affinity towards ETA receptors with an IC50 value of 1.4 nM and slightly lower affinity towards ETB receptors with an IC50 value of 600.0 nM. In the presence of ET1, it shows IC50 values of 3.1 nM and 1200.0 nM at ETA and ETB receptors, respectively. Moreover, it exhibits inhibitory activity towards human HDAC6 with a higher inhibition percentage of -52.55% using a commercial peptide substrate..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Avosentan(Ro 67-0565; SPP-301) is a potent endothelin receptor (ETA) antagonist with strong inhibitory effects on endothelin-1-induced contraction and may have protective effects against chronic kidney disease. [2]
Targets&IC50	ETA:3 nM
In vivo	METHODS: Avosentan (Ro 67-0565; SPP-301) was administered by intragastric administration in a single dose (6 rats per group: 0.1, 1.0, 10, 100 mg/kg). Rats were placed in metabolic cages for 24 hours after administration to assess body fluid electrolyte homeostasis. RESULTS The highest dose (100 mg/kg) of Avosentan (Ro 67-0565; SPP-301) resulted in reduced 24-hour diuresis (18.3%) and natriuresis (17.6%), hematocrit, and hematocrit in a hypertensive dTGR model Then it dropped. [1] METHODS: Apolipoprotein E (Apoe) knockout (KO) mice were randomly assigned to the following groups: nondiabetic controls and streptozotocin-induced diabetic animals treated daily with placebo, Avosentan (Ro 67-0565; SPP -301) (high dose: 30 mg/kg, or low dose: 10 mg/kg) by intragastric administration for 20 weeks. RESULTS Blood pressure remained unchanged after Avosentan (Ro 67-0565; SPP-301) treatment. High-dose Avosentan (Ro 67-0565; SPP-301) could significantly reduce diabetes-related albuminuria after 10 and 20 weeks of treatment. Creatinine clearance was normalized with Avosentan (Ro 67-0565; SPP-301). In diabetic mice, high-dose Avosentan (Ro 67-0565; SPP-301) treatment significantly attenuated the glomerulosclerosis index, mesangial matrix accumulation, glomerular accumulation of the matrix protein collagen IV, and the encoded connective tissue growth factor , renal expression of genes for vascular endothelial growth factor, transforming growth factor beta, and nuclear factor kappa B (p65 subunit). [2]
Synonyms	SPP-301, Ro 67-0565

Chemical Properties

Molecular Weight	479.51
Formula	C₂₃H₂₁N₅O₅S
Cas No.	290815-26-8
Smiles	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(nc1OC)-c1ccncc1
Relative Density.	1.364 g/cm3

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

H2O: Insoluble

DMSO: 45 mg/mL (93.85 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.09 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	2.0855 mL	10.4273 mL	20.8546 mL	104.2731 mL
5 mM	0.4171 mL	2.0855 mL	4.1709 mL	20.8546 mL
10 mM	0.2085 mL	1.0427 mL	2.0855 mL	10.4273 mL
20 mM	0.1043 mL	0.5214 mL	1.0427 mL	5.2137 mL
50 mM	0.0417 mL	0.2085 mL	0.4171 mL	2.0855 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 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