Preladenant, Adenosine A2A receptor antagonist (TBI4102)

Description

Product Details

Formal Name: 4-(Furan-2-yl)-10-[2-[4-[4-(2-methoxyethoxy)phenyl]piperazin-1-yl]ethyl]-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-7-amine

Alternate Names: SCH 420814

Molecular Formula: C₂₅H₂₉N₉O₃

Formula Weight: 503.57

CAS Number: 377727-87-2

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (5 mg/ml with warming)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Adenosine A2A receptor antagonist

Functions

Preladenant is a potent (Ki = 1.1nM) and selective (>1000-fold over other adenosine receptors) adenosine A2A antagonist. It has shown efficacy in rodent and primate models of Parkinsons disease without inducing dyskinesias and displays antidepressant effects. It has been shown that activation of the adenosine A2A receptor blocks the activation of immune cells and increases the number of regulatory T-cells. Currently in clinical trials as combination therapy with pembrolizumab.

Application Procedures

First dissolved in DMSO (5 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 1 month.