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Talarozole

Name: Talarozole
Brand: TargetMol
SKU: T7370
Price: 67 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7370Cas No. 201410-53-9

Alias R115866

Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) that inhibits CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively, for treating acne, psoriasis, and other keratinization disorders.

Talarozole

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Purity: 97.51%

Catalog No. T7370Alias R115866Cas No. 201410-53-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$67	In Stock	In Stock
5 mg	$137	In Stock	In Stock
10 mg	$177	In Stock	In Stock
25 mg	$248	In Stock	In Stock
50 mg	$322	In Stock	In Stock
100 mg	$488	-	In Stock
1 mL x 10 mM (in DMSO)	$148	In Stock	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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Purity:97.51%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Talarozole AI Summary

Talarozole shows potent inhibition of human CYP26B1 and CYP26A1 enzymes, with IC50 values of 0.46 nM and 5.1 nM, respectively, and effectively inhibits the metabolism of 9-cis-RA, as indicated by HPLC analyses in the presence of rat P450 reductase. This suggests its potential as a CYP26 inhibitor with implications for retinoic acid metabolism. Additionally, Talarozole exhibits antiviral activity against SARS-CoV-2 by inhibiting virus-induced cytotoxicity in both Caco-2 cells and VERO-6 cells at a concentration of 10 µM, though the inhibition rates varied across different assays and conditions. It inhibits SARS-CoV-2 3CL-Pro protease at 20 µM with inhibition rates reported between -0.02% and 20.95%. Despite varying IC50 values, some assays indicated values greater than 20,000 nM. The compound also shows inhibitory activity against human HDAC6 with inhibition percentages of 11.88% and 23.24% in enzymatic assays using different substrates, suggesting potential as an HDAC6 inhibitor. Talarozole additionally demonstrates cytotoxicity against human HepG2 cells, with an IC50 value of 14400 nM as assessed by the CellTiter-Glo luminescent cell viability assay..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) that inhibits CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively, for treating acne, psoriasis, and other keratinization disorders.
Targets&IC50	CYP26B1/A1:0.46/5.1 nM (IC50)
Synonyms	R115866

Chemical Properties

Molecular Weight	377.51
Formula	C₂₁H₂₃N₅S
Cas No.	201410-53-9
Smiles	CCC(CC)C(c1ccc(Nc2nc3ccccc3s2)cc1)n1cncn1
Relative Density.	1.26 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: 36 mg/mL (95.36 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (5.3 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	2.6489 mL	13.2447 mL	26.4894 mL	132.4468 mL
5 mM	0.5298 mL	2.6489 mL	5.2979 mL	26.4894 mL
10 mM	0.2649 mL	1.3245 mL	2.6489 mL	13.2447 mL
20 mM	0.1324 mL	0.6622 mL	1.3245 mL	6.6223 mL
50 mM	0.0530 mL	0.2649 mL	0.5298 mL	2.6489 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