Preladenant | Potent and selective adenosine A2A antagonist
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $70.00 | ||
| 25 mg | $240.00 |
Preladenant (377727-87-2) 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. 330 294
2) Hodgson et al. (2010), Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders; Exp.Neurol. 225 384
3) Pinna et al. (2016), Antidyskinetic effect of A2A and 5HT1A/B receptor ligands in two animal models of Parkinson’s disease; Mov.Disord. 31 501
4) Beavis et al. (2013), Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors; Proc.Natl.Acad.Sci USA. 110 14711
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. 29 90
6) Ohta et al. (2016), A metabolic immune checkpoint: adenosine in the tumor microenvironment; Front.Immunol. 7 1
7) NCT03099161
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Preladenant (377727-87-2) 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. 330 294
2) Hodgson et al. (2010), Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders; Exp.Neurol. 225 384
3) Pinna et al. (2016), Antidyskinetic effect of A2A and 5HT1A/B receptor ligands in two animal models of Parkinson’s disease; Mov.Disord. 31 501
4) Beavis et al. (2013), Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors; Proc.Natl.Acad.Sci USA. 110 14711
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. 29 90
6) Ohta et al. (2016), A metabolic immune checkpoint: adenosine in the tumor microenvironment; Front.Immunol. 7 1
7) NCT03099161
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