Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Tasimelteon (formerly BMS-214778; VEC-162; trade name: Hetlioz), a novel circadian regulator, is the first medication approved by both FDA and European Medicines Agency (EMA) for the treatment of Non-24-hour Sleep-Wake Disorder (Non-24), or sleep-wake disorder in blind individuals. Tasimelteon is a strong and selective agonist of the melatonin (MT1 and MT2) receptor that has a 2- to 4-fold higher affinity for the MT2 receptor. Tasimelteon therapy over the long term was risk-free and well-tolerated. Placebo-controlled data in patients with insomnia and those who are not 24 support this.
Targets |
MT2 receptor ( pKi = 9.8 ); MT1 receptor ( pKi = 9.45 )
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ln Vitro |
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ln Vivo |
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Animal Protocol |
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References |
Molecular Formula |
C15H19NO2
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Molecular Weight |
245.32
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Exact Mass |
245.14
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Elemental Analysis |
C, 73.44; H, 7.81; N, 5.71; O, 13.04
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CAS # |
609799-22-6
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Related CAS # |
Tasimelteon-d5; 1962124-51-1
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Appearance |
Solid powder
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SMILES |
N-[[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl]propanamide
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InChi Key |
PTOIAAWZLUQTIO-GXFFZTMASA-N
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InChi Code |
InChI=1S/C15H19NO2/c1-2-15(17)16-9-10-8-13(10)11-4-3-5-14-12(11)6-7-18-14/h3-5,10,13H,2,6-9H2,1H3,(H,16,17)/t10-,13+/m0/s1
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Chemical Name |
N-[[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl]propanamide
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO + Corn oil: 2.0mg/ml (8.15mM) |
Preparing Stock Solutions | 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 | |
10 mM | 0.4076 mL | 2.0382 mL | 4.0763 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05572281 | Active Recruiting |
Drug: Tasimelteon Oral Capsule Drug: Tasimelteon Oral Suspension |
Healthy | Vanda Pharmaceuticals | May 18, 2022 | Phase 1 |
NCT05361707 | Recruiting | Drug: Tasimelteon Oral Capsule, Tasimelteon Liquid Suspension |
Sleep Disorder Sleep Disturbance |
Vanda Pharmaceuticals | July 28, 2021 | Phase 3 |
NCT05922995 | Not yet recruiting | Drug: Tasimelteon | REM Behavior Disorder | Brigham and Women's Hospital | September 30, 2023 | Early Phase 1 |
NCT01477619 | Completed | Drug: Tasimelteon | Healthy Volunteers | Vanda Pharmaceuticals | November 2011 | Phase 1 |
NCT01540500 | Completed | Drug: Tasimelteon Drug: Fluvoxamine |
Healthy Volunteers | Vanda Pharmaceuticals | February 2012 | Phase 1 |
Mean plasma concentrations of tasimelteon (plotted on a semilogarithmic scale) after oral administration of 20 mg of tasimelteon to subjects with (A) mild (N = 8) or (B) moderate (N = 8) hepatic impairment and healthy matched controls (N = 8 for both groups). J Clin Pharmacol. 2015 May; 55(5): 525–533. td> |
Summary of AUC for tasimelteon and its metabolites after oral administration of 20 mg of tasimelteon to (A) subjects with mild or moderate hepatic impairment and healthy matched controls and (B) subjects with severe renal impairment or ESRD and healthy matched controls. J Clin Pharmacol. 2015 May; 55(5): 525–533. td> |
Mean plasma concentrations of tasimelteon after oral administration of single 20 mg doses of tasimelteon to subjects with ESRD (N = 8), subjects with severe impairment (N = 8), and matched controls (N = 8 for both groups)—linear (A) and semilogarithmic axes (B). Expert Opin Investig Drugs . 2011 Jul;20(7):987-93. td> |