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Tasimelteon

Name: Tasimelteon
Brand: TargetMol
SKU: T3495
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3495Cas No. 609799-22-6

Alias VEC-162, BMS-214778

Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

Tasimelteon

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Purity: 99.93%

Catalog No. T3495Alias VEC-162, BMS-214778Cas No. 609799-22-6

Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$38	In Stock	In Stock
25 mg	$68	In Stock	In Stock
50 mg	$113	In Stock	In Stock
100 mg	$189	In Stock	In Stock
500 mg	$473	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	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:99.93%

Color:White

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COA

Product Introduction

Tasimelteon AI Summary

Tasimelteon exhibits significant antiviral activity against SARS-CoV-2, showing a 28.66% inhibition of viral-induced cytotoxicity in Caco-2 cells at 10 μM concentration after 48 hours, as measured by high content imaging. It also inhibits SARS-CoV-2 3CL-Pro protease at 20 μM concentration, albeit with relatively low inhibition percentages of 7.34% and 1.176%. The compound's half-life in humans is 0.9 hours when administered at a 20 mg dose. Additionally, Tasimelteon demonstrates varied bioactivities in different cell types, notably in HEK293T cells where it enhances growth rates, and in U2OS and human fibroblast cells with mixed effects. It further interacts differentially with protein domains, modifying their thermal stability (Δ TM ranging from -1.55 C to 0.99 C), and shows inhibitory activity on multiple GPCRs, including C5AR1, APLNR, and S1PR1, suggesting potential pharmacological implications in GPCR signaling modulation. The compound also inhibits human HDAC6 activity with reduction percentages of 8.79% and 4.11% based on different peptide substrates..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.
Targets&IC50	MT2 receptor:9.8(pKi), MT1 receptor:9.45(pKi)
Synonyms	VEC-162, BMS-214778

Chemical Properties

Molecular Weight	245.32
Formula	C₁₅H₁₉NO₂
Cas No.	609799-22-6
Smiles	CCC(=O)NC[C@@H]1C[C@H]1c1cccc2OCCc12
Relative Density.	1.145 g/cm3

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 50 mg/mL (203.82 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.15 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	4.0763 mL	20.3815 mL	40.7631 mL	203.8154 mL
5 mM	0.8153 mL	4.0763 mL	8.1526 mL	40.7631 mL
10 mM	0.4076 mL	2.0382 mL	4.0763 mL	20.3815 mL
20 mM	0.2038 mL	1.0191 mL	2.0382 mL	10.1908 mL
50 mM	0.0815 mL	0.4076 mL	0.8153 mL	4.0763 mL
100 mM	0.0408 mL	0.2038 mL	0.4076 mL	2.0382 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