2. GPCR/G Protein Neuronal Signaling
  3. Melatonin Receptor
  4. Tasimelteon

Tasimelteon  (Synonyms: BMS-214778; VEC-162)

Cat. No.: HY-14803 Purity: 99.68%
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Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24).

For research use only. We do not sell to patients.

Tasimelteon Chemical Structure

Tasimelteon Chemical Structure

CAS No. : 609799-22-6

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 33 In-stock
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10 mg USD 48 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Tasimelteon:

Tasimelteon Related Antibodies

Top Publications Citing Use of Products

View All Melatonin Receptor Isoform Specific Products:

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MT1 MT2

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  • Purity & Documentation

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Description

Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].

IC50 & Target

MT2

 

In Vitro

Tasimelteon (BMS-214778) has 2.1-4.4 times greater affinity for the MT2 receptor believed to mediate circadian rhythm phase-shifting (Ki=0.0692 nM and Ki=0.17 nM in NIH-3T3 and CHO-K1 cells, respectively), than for the MT1 receptor (Ki=0.304 nM and Ki=0.35 nM, respectively). Tasimelteon has no appreciable affinity for more than 160 other pharmacologically relevant receptors and several enzymes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tasimelteon Related Antibodies
Clinical Trial
Molecular Weight

245.32

Formula

C15H19NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H][C@]1(C2=C3C(OCC3)=CC=C2)[C@@](CNC(CC)=O)([H])C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (134.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0763 mL 20.3815 mL 40.7631 mL
5 mM 0.8153 mL 4.0763 mL 8.1526 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0763 mL 20.3815 mL 40.7631 mL 101.9077 mL
5 mM 0.8153 mL 4.0763 mL 8.1526 mL 20.3815 mL
10 mM 0.4076 mL 2.0382 mL 4.0763 mL 10.1908 mL
15 mM 0.2718 mL 1.3588 mL 2.7175 mL 6.7938 mL
20 mM 0.2038 mL 1.0191 mL 2.0382 mL 5.0954 mL
25 mM 0.1631 mL 0.8153 mL 1.6305 mL 4.0763 mL
30 mM 0.1359 mL 0.6794 mL 1.3588 mL 3.3969 mL
40 mM 0.1019 mL 0.5095 mL 1.0191 mL 2.5477 mL
50 mM 0.0815 mL 0.4076 mL 0.8153 mL 2.0382 mL
60 mM 0.0679 mL 0.3397 mL 0.6794 mL 1.6985 mL
80 mM 0.0510 mL 0.2548 mL 0.5095 mL 1.2738 mL
100 mM 0.0408 mL 0.2038 mL 0.4076 mL 1.0191 mL
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Tasimelteon Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tasimelteon609799-22-6BMS-214778 VEC-162BMS214778BMS 214778VEC162VEC 162VEC-162Melatonin ReceptororallyDMRAMT2MT1circadianregulatorNon-24Inhibitorinhibitorinhibit

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