Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| CHO | EC50 | > 10000 nM | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method | [PMID: 25780876] |
| CHO | EC50 | 0.018 μM | Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting | [PMID: 23245803] |
| CHO | EC50 | 0.04 μM | G-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assay | [PMID: 11784146] |
| CHO | EC50 | 10.2 nM | Agonist activity at human recombinant adenosine receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 45 mins prior forskolin-induction measured after 15 mins by immunoassay | [PMID: 21858244] |
| CHO | EC50 | 12.58 nM | Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method | [PMID: 25780876] |
| CHO | EC50 | 30 nM | Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay | [PMID: 20031406] |
| CHO | EC50 | 38 nM | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay | [PMID: 20031406] |
| CHO | EC50 | 45 nM | Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay | 10.1039/C5MD00086F |
| CHO | EC50 | 63 nM | Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay | [PMID: 20031406] |
| CHO-K1 | EC50 | 17.6 nM | Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay | [PMID: 24900277] |
| COS-7 | EC50 | 0.078 μM | Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay | [PMID: 16640329] |
| COS-7 | EC50 | 10.4 μM | Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay | [PMID: 16640329] |
| HCT-116 | IC50 | > 10 μM | Cytotoxicity against human HCT-116 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay | [PMID: 35707146] |
| HEK293 | EC50 | 188 nM | Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis | [PMID: 32271569] |
| HEK293 | IC50 | 3.7 x 10 | Displacement of [3H]CGS 21680 from human recombinant adenosine receptor A2A expressed in HEK293 cells measured after 120 mins by scintillation counting method | [PMID: 27876250] |
| PBMC | IC50 | 187 nM | Antiinflammatory activity in rat PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA | [PMID: 20031406] |
| PBMC | IC50 | 40 nM | Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA | [PMID: 20031406] |
| PC-12 | EC50 | 130 nM | Potency against PC12 cell A2 adenosine receptor by adenylate cyclase activation | [PMID: 3018244] |
| PC-3 | IC50 | > 10 μM | Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay | [PMID: 35707146] |
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