Adenosine Kinase Inhibitor (hydrate)

IC50: 1.7 nM in cell-free assays Adenosine Kinase Inhibitor is an inhibitor of adenosine kinase. Adenosine kinase is the key metabolizing enzyme regulating cellular adenosine concentrations. Inhibition of adenosine kinase can selectively enhance the protective actions of adenosine during tissue trauma without producing the nonspecific effects associated with the systemic administration of adenosine receptor agonists. In vitro: Adenosine Kinase Inhibitor was found to be a potent non-nucleoside adenosine kinase inhibitor with several folds of magnitude selectivity over other sites of adenosine interaction. Adenosine Kinase Inhibitor was 1300- to 7700-fold selective for adenosine kinase compared with other neurotransmitter and peptide receptors, neurotransmitter/nucleoside reuptake sites, and enzymes. Adenosine Kinase Inhibitor was equipotent in inhibiting native human adenosine kinase, human recombinant isoforms, as well as adenosine kinase from dog, rat, monkey, and mouse brain . In vivo: Adenosine Kinase Inhibitor was orally active and efficacious in reducing acute somatic nociception in the mouse hot-plate assay. Adenosine Kinase Inhibitor could dose-dependently reduce nociception in the phenyl-p-quinone-induced abdominal constriction assay. The antinociceptive effects of Adenosine Kinase Inhibitor in the hotplate assay were stop by the nonselective adenosine receptor antagonist theophylline, but not by a peripherally selective adenosine receptor antagonist . Clinical trial: So far, no clinical study has been conducted.

Product information

Molecular Weight: 481.35

Formula: C22H21BrN6O2

Chemical Name: 5-(3-bromophenyl)-7-[6-(morpholin-4-yl)pyridin-3-yl]pyrido[2,3-d]pyrimidin-4-amine hydrate

Smiles: O.NC1=NC=NC2N=C(C=C(C=21)C1=CC(Br)=CC=C1)C1=CN=C(C=C1)N1CCOCC1

InChiKey: GGSVVLZSNMFBHH-UHFFFAOYSA-N

InChi: InChI=1S/C22H19BrN6O.H2O/c23-16-3-1-2-14(10-16)17-11-18(28-22-20(17)21(24)26-13-27-22)15-4-5-19(25-12-15)29-6-8-30-9-7-29;/h1-5,10-13H,6-9H2,(H2,24,26,27,28);1H2

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

Products are for research use only. Not for human use.