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CGS 21680

Cat. No. M3228
CGS 21680 Structure
Size Price Availability
10mg USD 120  USD120 Out of stock
25mg USD 250  USD250 Out of stock
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Quality Control & Documentation
Biological Activity

CGS 21680 is a specific adenosine (A2A) subtype receptor agonist with an IC50 of 5.6 μM for reducing input resistance of the membrane potential. The Ki of CGS 21680 adenosine (A2A) subtype receptor is 27 nM. CGS 21680 has less affinity for A1 and A3 adenosine receptors than A2A- and A2B subtype. CGS 21680 starting at the onset of arthritis (Day 25) improved the clinical signs at Days 26-35 and ameliorated histological states in the joint and paw. The degree of oxidative and nitrosative damage was markedly decreased in CGS 21680-treated mice as exhibited by increased contents of malondialdehyde, formation of nitrotyrosine, and activation of poly (ADP-ribose) polymerase. Plasma levels of proinflammatory cytokines including tumor necrosis factor, interleukin 1ß (IL-1ß) and IL-6 were also decreased by CGS 21680. CGS 21680 also reduced the expression of inducible nitric oxide synthase and cyclooxygenase-2.

Product Citations
Customer Product Validations & Biological Datas
Source PLoS One (2018). Figure 5. CGS 21680
Method Immunizations
Cell Lines WT mice
Concentrations 1 mg/kg
Incubation Time four weeks
Results We thus investigated whether administration of an A2a adenosine receptor agonist (CGS 21680) could enhance antibody responses following Pneumovax 23 vaccination in young mice. As shown in Fig 5A and 5B, treatment with the A2a agonist significantly increased mean IgG3 levels at day 7 and 14 post-vaccination
Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models rat
Formulation water
Dosages 10 mg/kg
Administration p.o.
Chemical Information
Molecular Weight 499.52
Formula C23H29N7O6
CAS Number 120225-54-9
Solubility (25°C) DMSO 77 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Russell W Brown, et al. The adenosine A(2A) receptor agonist CGS 21680 alleviates auditory sensorimotor gating deficits and increases in accumbal CREB in rats neonatally treated with quinpirole

[2] Dionisio A Amodeo, et al. The adenosine A 2A receptor agonist, CGS 21680, attenuates a probabilistic reversal learning deficit and elevated grooming behavior in BTBR mice

[3] Emanuela Mazzon, et al. CGS 21680, an agonist of the adenosine (A2A) receptor, reduces progression of murine type II collagen-induced arthritis

[4] Daniela Impellizzeri, et al. CGS 21680, an agonist of the adenosine (A2A) receptor, decreases acute lung inflammation

[5] M F Jarvis, et al. [3H]CGS 21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain

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