Name | DH97 |
---|---|
Synonyms |
Pentanamide, N-[2-[2-(phenylmethyl)-1H-indol-3-yl]ethyl]-
N-(2-(2-Benzyl-1H-indol-3-yl)ethyl)pentanamide N-[2-(2-Benzyl-1H-indol-3-yl)ethyl]pentanamide DH97 MFCD02262121 |
Description | DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. DH97 shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses[1][2]. |
---|---|
Related Catalog | |
Target |
MT2:8.03 (pKi) MT1:6.08 (pKi) |
In Vitro | DH97 (compound 9) (0.1-100 μM; 2 h) antagonizes pigment aggregation induced by melatonin (10 nM) in Xenopus laevis melanophores[1]. DH97 has no agonist activity at concentrations up to 100 µM[1]. DH97 (60 nM) significantly alteres the potency of melatonin in the rat tail artery at low concentrations of the MT2 selective ligands, with a pEC50 of 8.83[2]. DH97 (5 μM) causes a significant rightward displacement of the vasoconstrictor effect of melatonin at concentrations non-selective for mt1 and MT2 receptors[2]. |
References |
Density | 1.1±0.1 g/cm3 |
---|---|
Boiling Point | 580.1±38.0 °C at 760 mmHg |
Molecular Formula | C22H26N2O |
Molecular Weight | 334.455 |
Flash Point | 304.6±26.8 °C |
Exact Mass | 334.204498 |
LogP | 4.63 |
Vapour Pressure | 0.0±1.6 mmHg at 25°C |
Index of Refraction | 1.605 |