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Preladenant | Potent and selective adenosine A2A antagonist

Preladenant is a potent (Ki = 1.1nM) and selective (>1000-fold over other adenosine receptors) adenosine A2A antagonist.1 It has shown efficacy in rodent and primate models of Parkinsons disease without inducing dyskinesias and displays antidepressant effects.1-3 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.4-6 Currently in clinical trials as combination therapy with pembrolizumab.7

References/Citations
1) Hodgson et al. (2009), Characterization of the potent and selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimodin-5-amine] in rat models of movement disorders and depression; J.Pharmacol.Exp.Ther. 330294
2) Hodgson et al. (2010), Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders; Exp.Neurol. 225384
3) Pinna et al. (2016), Antidyskinetic effect of A2A and 5HT1A/B receptor ligands in two animal models of Parkinson’s disease; Mov.Disord. 31501
4) Beavis et al. (2013), Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors; Proc.Natl.Acad.Sci USA. 11014711
5) Hatfield and Sitkovsky (2016), A2A adenosine receptor antagonist to weaken the hypoxia-HIF-1a driven immunosuppression and improve immunotherapies of cancer; Curr.Opin.Pharmacol. 2990
6) Ohta et al. (2016), A metabolic immune checkpoint: adenosine in the tumor microenvironment; Front.Immunol. 71
7) NCT03099161


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Catalog#  10-4102-0005

$65.00
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CAS:
377727-87-2
Catalog Number:
10-4102
Chemical 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 Name:
SCH 420814
Molecular Weight:
503.57
Molecular Formula:
C29H29N9O3
Solubility:
Soluble in DMSO (up to 5 mg/ml with warming).
Physical Properties:
Beige solid
Purity:
>98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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