- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S2790||Istradefylline||<1 mg/mL||6 mg/mL||<1 mg/mL|
|S2153||CGS 21680 HCl||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S8575||A2AR antagonist 1||<1 mg/mL||61 mg/mL||<1 mg/mL|
|S8105||ZM241385||<1 mg/mL||67 mg/mL||<1 mg/mL|
|S8314||5-Iodotubercidin||<1 mg/mL||78 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|
- Adenosine Receptor Inhibitors (7)
- New Adenosine Receptor Products
|Catalog No.||Information||Product Use Citations||Product Validations|
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)
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.
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.
ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.
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.
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.