Inosine-2,8-d2 is the deuterium labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors[1][2][3].
SCH 58261 is the adenosine A2A receptor competitive antagonist. Displays 323-, 53- and 100-fold selectivity over A1, A2B and A3 receptors, respectively.target: adenosine A2A receptorIC50: 15 nM [3]in vitro: NK cells were cultured in NK cell media and preincubated with or without 1 uM SCH58261 30 min before simulation with indicated concentrations of IL-18 (R & D Systems) and IL-12p70 (Australian Biosearch) in the presence or absence of NECA (1 uM) or CGS-21680 (100 nM).[1]in vivo: it was demonstrated that the selective antagonist of the A2Areceptor, SCH58261, administered i.p. starting from the early minutes after ischemia induction, reduces ischemic brain damage and neurological deficit 24 h thereafter. vehicle-rats received saline with Tween 80 (1 %) administered (i.p.) .SCH58261 (0.01 mg/kg, i.p.), administered twice/day for 7 days [2]
Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease[1][2][3].
N-0861 racemate is the racemate of N-0861. N-0861 is a selective adenosine A1 receptor antagonist.
ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease[1][2].
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research[1][2][3].
Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity[1].
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].
CPI-444 is a potent and selective inhibitor of A2A receptor (A2AR) induces antitumor responses.
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease[1][2].
IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent[1].
(Rac)-Mirabegron D5 ((Rac)-YM178 D5) is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist[1].
ST4206 is a potent adenosine A2A antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively.
LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
KFM19 is a potent, selective Adenosine receptor (A1-receptor) antagonist, with an IC50 of 50 nM.
A1AR antagonist 4 (compound 22) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.51 and a pKi of 6.29[1].
Vipadenant is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.
N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively[1].
UP202-56 is an adenosine analogue, which is an adenosinergic agonist.
Adenosine 5'-monophosphate monohydrate is an adenosine A1 receptor agonist.
ZM 241385 is a selective and high affinity A2A adenosine receptor antagonist.
CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively[1].
ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
TC-G 1004 (compound 16j) is an orally active A2A adenosine receptor antagonist, with Ki values of 0.44 nM and 80 nM for hA2A and hA1, respectively[1].
Adenosine 5'-monophosphate disodium is an orally active purine nucleotide, and participates in ATP metabolism. Adenosine 5'-monophosphate disodium is also a ligand for adenosine 2B receptor. Adenosine 5'-monophosphate disodium can activate AMPK in skeletal muscle, and ameliorates insulin resistance and impaired glucose metabolism. Adenosine 5'-monophosphate disodium can be used for research of diabetes[1][2][3].
A2B receptor antagonist 2 (compound 18) is an adenosine receptor A2B antagonist, with Ki values of 2.30 μM, 6.8 μM and 3.44 μM for rA1, rA2A and hA2B, respectively[1].
Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation[1][2].
Piclidenoson (IB-MECA) is an agonist of the adenosine A3 receptor with EC50 values of 0.11 μM. IC50 value: 0.11 μM (EC50) [3]Target: adenosine A3 receptorin vitro: Piclidenoson has been shown to play important roles in cell proliferation and apoptosis in a variety of cancer cell lines. ThePiclidenoson was capable of decreasing intracellular cyclic adenosine monophosphate (cAMP) that was the reason for the presence of functional A3 adenosine receptor on the cell lines. Piclidenoson significantly reduced cell viability in a dose-dependent manner. Piclidenoson, an A3AR agonist, inhibits the growth of different cancer cell types like melanoma, colon, breast, leukemia, and prostatePiclidenoson was able to inhibit forskolin-stimulated cAMP levels with an EC50 value of 0.82 μM in OVCAR-3 cells. Piclidenoson was able to inhibit forskolin-stimulated cAMP levels with an EC50 value of 1.2 μM in Caov-4 cells.in vivo: Administrations of single intraperitoneal doses of either Piclidenoson 0.5 h post-irradiation resulted in statistically significant increases of MST in comparison with the control irradiated mice.[2]
N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM). IC50 value: 8.2 nM (EC50)Target: A1 receptorin vivo: N6-Cyclohexyladenosine exerts anticonvulsant effects and protects against neuronal death. CHA was also found to inhibit the pressor effects of lumbar sympathetic nerve stimulation in rats.