220339-00-4

220339-00-4 structure
220339-00-4 structure
  • Name: DH 97
  • Chemical Name: DH97
  • CAS Number: 220339-00-4
  • Molecular Formula: C22H26N2O
  • Molecular Weight: 334.455
  • Catalog: Signaling Pathways GPCR/G Protein Melatonin Receptor
  • Create Date: 2018-06-12 22:00:30
  • Modify Date: 2025-08-25 15:15:19
  • 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].

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

[1]. Teh MT, et, al. Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophores. Naunyn Schmiedebergs Arch Pharmacol. 1998 Nov;358(5):522-8.

[2]. Ting KN, et, al. Molecular and pharmacological evidence for MT1 melatonin receptor subtype in the tail artery of juvenile Wistar rats. Br J Pharmacol. 1999 Jun;127(4):987-95.

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
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