1. GPCR/G Protein Neuronal Signaling
  2. Melatonin Receptor
  3. DH97

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.

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DH97 Chemical Structure

DH97 Chemical Structure

CAS No. : 220339-00-4

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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].

IC50 & Target[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

334.45

Formula

C22H26N2O

CAS No.
SMILES

CCCCC(NCCC1=C(CC2=CC=CC=C2)NC3=C1C=CC=C3)=O

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DH97
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HY-107628
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