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AC-261066

Name: AC-261066
Brand: TargetMol
SKU: T14089
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14089Cas No. 870773-76-5

Alias AC 261066

AC-261066 is an orally available and isoform-selective agonist of RARβ2 with a pEC50 of 8.0.

AC-261066

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Purity: 99.64%

Catalog No. T14089Alias AC 261066Cas No. 870773-76-5

AC-261066 is an orally available and isoform-selective agonist of RARβ2 with a pEC50 of 8.0.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	-	In Stock
5 mg	$58	-	In Stock
10 mg	$106	-	In Stock
25 mg	$238	-	In Stock
50 mg	$353	-	In Stock
100 mg	$495	-	In Stock
1 mL x 10 mM (in DMSO)	$69	-	In Stock

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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.

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Batch Information

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Purity:99.64%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR LCMS

Product Introduction

AC-261066 AI Summary

AC-261066 is a potent and selective modulator of retinoic acid receptors, demonstrating high efficacy against RARbeta2 (96.0% with EC50 of 10.0 nM) and RARgamma-LBD (EC50 of 5.8 nM). It shows moderate efficacy against RARbeta1, and pharmacological activity against RARalpha, and RARgamma. Known for its good metabolic stability in human and rat liver microsomes, it presents with a clearance rate of 36.0 mL.min-1.g-1 in humans and 10.0 mL.min-1.g-1 in rats. The compound is characterized by a high partition coefficient (log P = 5.1), a moderate distribution coefficient (log D = 1.4), and high aqueous solubility at pH 7.4 (4800.0 ug.mL-1). It exhibits favorable oral bioavailability (52.0%) in rats and a considerable clearance rate of 41.0 mL.min-1.kg-1. Additionally, AC-261066 demonstrates antiviral properties, effectively inhibiting SARS-CoV-2 induced cytotoxicity in various cell types and showing inhibitory activity against the SARS-CoV-2 3CL-Pro protease (100.6% inhibition at 20 μM). It also impacts cell proliferation assays in many cell lines, including anti-cancer activities and potential inhibition of Yes1 kinase. Furthermore, the compound influences RARbeta2 mRNA expression in human BE(2)-C cells and modifies the thermal stability of specific protein domains. Overall, AC-261066 exhibits a diverse profile of bioactivities, ranging from receptor modulation to antiviral and anti-cancer activities, making it a promising candidate for further drug development..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	AC-261066 is an orally available and isoform-selective agonist of RARβ2 with a pEC50 of 8.0.
Targets&IC50	RARβ2:8.0 （pEC50）
Synonyms	AC 261066

Chemical Properties

Molecular Weight	353.41
Formula	C₁₇H₂₀FNO₄S
Cas No.	870773-76-5
Smiles	CCCCOCCOc1nc(sc1C)-c1ccc(C(O)=O)c(F)c1
Relative Density.	1.247 g/cm3 (Predicted)

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: 40 mg/mL (113.18 mM), Sonication and heating to 80℃ are recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8296 mL	14.1479 mL	28.2957 mL	141.4787 mL
5 mM	0.5659 mL	2.8296 mL	5.6591 mL	28.2957 mL
10 mM	0.2830 mL	1.4148 mL	2.8296 mL	14.1479 mL
20 mM	0.1415 mL	0.7074 mL	1.4148 mL	7.0739 mL
50 mM	0.0566 mL	0.2830 mL	0.5659 mL	2.8296 mL
100 mM	0.0283 mL	0.1415 mL	0.2830 mL	1.4148 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