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.
Product information
CAS Number: 220339-00-4
Molecular Weight: 334.45
Formula: C22H26N2O
Chemical Name: (Z)-N-[2-(2-benzyl-1H-indol-3-yl)ethyl]pentanimidic acid
Smiles: CCCC/C(/O)=N/CCC1C2=CC=CC=C2NC=1CC1C=CC=CC=1
InChiKey: HDOIPCLEKCEANF-UHFFFAOYSA-N
InChi: InChI=1S/C22H26N2O/c1-2-3-13-22(25)23-15-14-19-18-11-7-8-12-20(18)24-21(19)16-17-9-5-4-6-10-17/h4-12,24H,2-3,13-16H2,1H3,(H,23,25)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
DH97 (compound 9) (0.1-100 μM; 2 h) antagonizes pigment aggregation induced by melatonin (10 nM) in Xenopus laevis melanophores. DH97 has no agonist activity at concentrations up to 100 µM. 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. DH97 (5 μM) causes a significant rightward displacement of the vasoconstrictor effect of melatonin at concentrations non-selective for mt1 and MT2 receptors.
Products are for research use only. Not for human use.
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