- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S8314||5-Iodotubercidin||<1 mg/mL||78 mg/mL||<1 mg/mL|
|S2790||Istradefylline||<1 mg/mL||6 mg/mL||<1 mg/mL|
|S8575||A2AR antagonist 1||<1 mg/mL||61 mg/mL||<1 mg/mL|
|S5427||Alloxazine||-1 mg/mL||2 mg/mL||-1 mg/mL|
|S4932||Proxyphylline||-1 mg/mL||47 mg/mL||-1 mg/mL|
|S3988||Theophylline-7-acetic acid||-1 mg/mL||47 mg/mL||-1 mg/mL|
|S8105||ZM241385||<1 mg/mL||67 mg/mL||<1 mg/mL|
|S8104||SCH58261||<1 mg/mL||69 mg/mL||<1 mg/mL|
|S7588||Reversine||<1 mg/mL||5 mg/mL||<1 mg/mL|
|S2153||CGS 21680 HCl||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S1647||Adenosine||<1 mg/mL||12 mg/mL||<1 mg/mL|
|S5358||Regadenoson||<1 mg/mL||56 mg/mL||56 mg/mL|
- Adenosine Receptor Inhibitors (13)
- New Adenosine Receptor Products
|Catalog No.||Information||Product Use Citations||Product Validations|
5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.
Istradefylline is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.
The effect of caffeine (CAF) and adenosine A1 and A2A receptor antagonists, DPCPX and KW 6002 (KW) on DA release induced by MDMA in the mouse striatum.KW (1.25 and 2.5 mg/kg) were injected simultaneously with MDMA 20 or 40 mg/kg as indicated with an arrow. Values are the mean ± SEM (n = 6–8 animals). *P < 0.0001 represents a significant difference in comparison to control group; “a” P < 0.0002 represents a significant difference in comparison to MDMA group (repeated measures ANOVA and Tukey’s post-hoc test)
A2AR antagonist 1 is a potent A2AR (Adenosine A2A Receptor) antagonist with Ki values of 4 nM and 264 nM for A2AR and A1R, respectively.
Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.
AZD-4635 (HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors.
Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 µM for platelets).
Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class.
ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.
T cells treated with MTX, astilbin, ZM241385 and SCH772984. The levels of p-ERK1/2, p-P65, p-STAT1 and p-STAT3 were analyzed by western blot.
SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
Immunofluorescence of acetylated a-tubulin (red) in control (a), reversin-treated (b), and BI 2536/Reversin mixture-treated embryos (c).The embryos treated with Reversine completed first mitosis, but the nuclei of their blastomeres were fragmented (b, arrows). Embryos inhibited withthe BI 2536/Reversine mixture arrested before the onset of anaphase. Microtubules of the spindle are disorganized (c, double-arrow) and thechromosomes are misaligned (c, arrows) in these inhibited embryos. DNA is counter-stained with DAPI (blue). Scale bar, 10 μm.
CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
Effects of CGS-21,680 and forskolin on caffeine inhibited the expression of leptin in the human BeWo cells. The cells were treated with CGS-21,680 (2 μM, adenosine receptor A2a (ADORA2A) agonist)/forskolin (4 μM, adenylyl cyclase (AC) agonist, cAMP activator) and/or caffeine (20 μM) for 7 d. (A and B) The mRNA expression of leptin and ADORA2A was detected by quantitative real-time PCR, n = 3. (C) The protein expression of ADORA2A was detected by Western blotting, n = 2. (D) At the end of the treatment, the mRNA expression of leptin was detected by real-time PCR, n = 3. GAPDH was used as an internal control. The results are expressed as the mean ± S.E.M. of three independent experiments; *P < 0.05 and **P < 0.01 vs. control.
Adenosine is a nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond.
Regadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity.