Tasimelteon | B2985

Tasimelteon is a potent Dual Melatonin Receptor Agonist (DMRA). It is used to treat non-24-hour sleep-wake disorder. The Ki values for binding affinity at melatonin receptors MT1 and MT2 receptor are 0.304 and 0.069 nM respectively in CHO–K1 cells. It shows greater affinity for the MT2 receptor which is believed to mediate circadian rhythm phase-shifting. It induces a potent, concentration-dependent inhibition of forskolin-stimulated cAMP accumulation in NIH-3T3 cells stably expressing human MT1 and MT2 receptors with EC₅₀ values of 0.74 nM and 0.1 nM repectively.

Tasimelteon is a potent Dual Melatonin Receptor Agonist (DMRA). It is used to treat non-24-hour sleep-wake disorder. The Ki values for binding affinity at melatonin receptors MT1 and MT2 receptor are 0.304 and 0.069 nM respectively in CHO–K1 cells. It shows greater affinity for the MT2 receptor which is believed to mediate circadian rhythm phase-shifting. It induces a potent, concentration-dependent inhibition of forskolin-stimulated cAMP accumulation in NIH-3T3 cells stably expressing human MT1 and MT2 receptors with EC₅₀ values of 0.74 nM and 0.1 nM repectively.

B2985 | Tasimelteon DataSheet

Alternate Name/Synonyms: N-[[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl]propanamide; Hetlioz; BMS 214778; VEC-162; MA 1; (1R-trans)-N-[[2-(2,3-Dihydro-4-benzofuranyl)cyclopropyl]methyl]propanamide

Appearance: White to Off-White powder

Formulation:

CAS Number: 609799-22-6

Structure Available?: True

Peptide sequence:

Salt Form: False

Molecular Formula: C₁₅H₁₉NO₂

Molecular Weight: 245.32

Cell-Permeable?: False

Purity: 0.95

Solubilities: ~2 mg/ml in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A potent Dual Melatonin Receptor Agonist (DMRA)

MDL Number: MFCD09033789

PubChem CID: 10220503

SMILES: CCC(=O)NCC1CC1C2=C3CCOC3=CC=C2

InChi: 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

InChi Key: PTOIAAWZLUQTIO-GXFFZTMASA-N