Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues. These receptors have distinct localization, signal transduction pathways and different means of regulation upon exposure to agonists. A key property of some of Adenosine receptors is their ability to serve as sensors of cellular oxidative stress, which is transmitted by transcription factors, such as NF-κB, to regulate the expression of ARs. The importance of Adenosine receptors in the regulation of normal and pathological processes such as sleep, the development of cancers and in protection against hearing loss will be examined.
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A potent and selective A2A adenosine receptor with Ki of 1.3 nM; displays 50-fold selectivity over A1 and A2B, and no activity against A3, P450 isoforms and hERG; shows excellent preclinical pharmacokinetics, and demonstrates strong oral activity in commonly used models of Parkinson's disease.
ZM-241385 is a potent, non-xanthine A2A selective adenosine receptor antagonist with rat PC12 binding pIC50 of 9.52; shows low affinity for A3 (pIC50=3.82); antagonizes vasodilatation of the coronary bed produced by 2-CADO and CGS21680 with pA2 of 8.57 and 9.02, respectively, in guinea-pig isolated Langendorff hearts; selectively attenuates the mean arterial blood pressure response produced by exogenous adenosine in conscious spontaneously hypertensive rats (3-10 mg/kg, p.o.).
2-Cl-IB-MECA (Chloro-IB-MECA, CF-102, Namodenoson) is a potent, selective A3 adenosine receptor agonist with Ki of 0.33 nM, 2500- and 1400-fold selectivity over A1 and A2a receptors; also displays 46,000-fold selectivity versus the Na(+)-independent adenosine transporter; inhibits adenylate cyclase via rat A3 receptors in CHO cells (IC50=67 nM); induces apoptosis in HL-60 cells at concentrations of <30 uM, significantly induced Ca(2+) release from intracellular Ca(2+) pools followed by Ca(2+) influx; increases plasma histamine concentrations in conscious rats.
AB928 (AB-928) is a potent, dual antagonist of the A2aR and A2bR adenosine receptors with Kb of 1.5 and 2.0 nM, respectively; displays high selectivity towards related receptors (A1R, A3R, CD73, CD39, NTPDase 2/3); AB928 is a potent inhibitor of NECA-mediated A2aR activation on cell lines, potently reverses adenosine-mediated CD8+ T cell suppression, potently inhibits cAMP-mediated pCREB activation in human leukocyte populations in whole blood; inhibits tumor micro-environment adenosine generation and signaling for the treatment of cancer.
MRS1186 (MRS-1186) is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist with Ki of 7.66 nM.
KH-176 (KH176, Sonlicromanol) is a smal molecule ROS-redox modulator, effectively reduces increased cellular ROS levels and protects OXPHOS deficient primary cells against redox perturbation by targeting the Thioredoxin/Peroxiredoxin system; significantly improves rotarod and gait performance and reduces the degeneration of retinal ganglion cells in Ndufs4 -/- mice, shows therapeutic effects in mammalian model of Leigh Disease.
Taminadenant is an adenosine receptor A2a antagonist.
AZD-4635 (HTL 1071) is a potent, selective and orally available adenosine 2A receptor (A2AR) inhibitor with Ki of 1.7 nM, > 30-fold selectivity over other adenosine receptors; reverses the inhibitory effects of different concentrations of adenosine in CHO cells stably expressing human A2AR with IC50 of 0.1 nM (incubated with 0.1 uM adenosine); reverses suppression and restores IFNγ secretion in cells incubated with NECA in ex vivo CD8+ T cell assay; reduces tumor burden and enhances antitumor immunity in vivo.
A potent, orally active, adenosine A2A receptor antagonist that is being investigated in solid tumors as a single agent and in combination with the anti-PD-L1 antibody atezolizumab; dose-dependent inhibits tumor growth in mouse model MC38; induces anti-tumor immunity in mouse tumor models and inhibits adenosine signaling in lymphocytes of treated humans.
A potent and highly selective A2A receptor competitive antagonist with Ki of 1.1 nM; has >1000-fold selectivity over all other adenosine receptors; attenuates hypolocomotion induced by the A2AR agonist CGS-21680; potentiates L-Dopa -induced contralateral rotations after 6-hydroxydopamine lesions in the medial forebrain bundle in rats (0.1-1 mg/kg); orally active.
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