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Submit ReviewTasimelteon is a high affinity and selective dual melatonin receptor (MT1/MT2) agonist (Ki values are 0.304 nM and 0.0692 nM, respectively). It has no significant interaction with any other commonly screened receptors or enzyme binding sites. Tasimelteon induces a potent, concentration-dependent inhibition of forskolin-stimulated cAMP accumulation in NIH-3T3 cells stably expressing human MT1 (EC50 = 0.74 nM) or expressing human MT2 (EC50 = 0.1 nM) receptors. Tasimelteon is a circadian regulator.
分子量 | 245.32 |
公式 | C15H19NO2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 609799-22-6 |
PubChem ID | 10220503 |
InChI Key | PTOIAAWZLUQTIO-GXFFZTMASA-N |
Smiles | CCC(NC[C@@H]1C[C@H]1C2=C(CCO3)C3=CC=C2)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 24.53 | 100 | |
ethanol | 24.53 | 100 |
以下数据基于产品分子量 245.32。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 4.08 mL | 20.38 mL | 40.76 mL |
5 mM | 0.82 mL | 4.08 mL | 8.15 mL |
10 mM | 0.41 mL | 2.04 mL | 4.08 mL |
50 mM | 0.08 mL | 0.41 mL | 0.82 mL |
参考文献是支持产品生物活性的出版物。
Lavedan et al (2015) Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology 91 142 PMID: 25534555
Vachharajani et al (2003) Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist. J.Pharm.Sci. 92 760 PMID: 12661062
If you know of a relevant reference for Tasimelteon, please let us know.
关键词: Tasimelteon, Tasimelteon supplier, Potent, selective, dual, melatonin, receptors, MT1, MT2, agonists, circadian, rhythm, regulators, Melatonin, (MT), Receptors, 7493, Tocris Bioscience
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