CGS 21680 HCl
Molecular Weight(MW): 535.98
CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
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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.
Toxicol Appl Pharmacol, 2016, 289(1):109-16.. CGS 21680 HCl purchased from Selleck.
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Choose Selective Adenosine Receptor Inhibitors
|Description||CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.|
CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor. In an isolated perfused working rat heart model, CGS 21680C effectively increases coronary flow with an ED25 value of 1.8 nM.  CGS 21680 binds adenosine A2 receptor with high affinity (Kd = 15.5 nM) and limited capacity (apparent Bmax = 375 fmol/mg of protein) to a single dass of recognition sites. In hippocampal slices, CGS 21680 apis weak agonist on pre- and postsynaptic measures of electrophysiologicaJ activity (putative Al receptor mediated events) and is ineffective at stimulating the formation of cAMP (a putative A2 mediated response). In striatal slices, CGS 21680 potently stimulates the formation of cAMP with an EC50 of 110 nM but is ineffective at inhibiting electrically stimulated dopamine release. CGS 21680A is the hydrochloride salt, while CGS 21680C is the sodium salt of CGS 21680.
|In vivo||CGS 21680A is active p.o. in the spontaneously hypertensive rat at a dose of 10 mg/kg with efficacy for up to 24 hr. CGS 21680A caused a transient (60 min) increase in heart rate. CGS 21680 is a potent depressant of the spontaneous, acetylcholine and glutamate evoked firing of rat cerebral cortical neurons. |
|In vitro||DMSO||107 mg/mL (199.63 mM)|
|In vivo||30% propylene glycol, 5% Tween 80, 65% D5W||30 mg/mL|
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