CGS 21680 |
| Catalog No.GC10172 |
CGS 21680 is a selective adenosine A2A receptor agonist with an IC50 value of 22nM. This product is in free form, which is unstable, we recommend the stable salt form CGS 21680 Hydrochloride (GC11978) with the same biological activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120225-54-9
Sample solution is provided at 25 µL, 10mM.
CGS 21680 is a selective adenosine A2A receptor agonist with an IC50 value of 22nM[1]. This product is in free form, which is unstable, we recommend the stable salt form CGS 21680 Hydrochloride (GC11978) with the same biological activity. CGS 2168 enhances the release of excitatory transmitter amino acids in the ischemic rat cerebral cortex[2]. CGS 21680 accelerates the resequestration of cytoplasmic calcium and inhibits the proinflammatory activity of human neutrophils[3].
In vitro, CGS 21680 (1µM) treatment of human urothelial cell line (UROtsa cells) and human neutrophils for 3h significantly reduced cell migration induced by uropathogenic Escherichia coli (UPEC)[4].
In vivo, CGS 21680 (0.1mg/kg) treated humanized NSG mice by intraperitoneal injection had a dual effect, increasing weight loss, reducing T cells, and increasing serum human IL-6 concentrations, but reducing hepatic leukocyte infiltration and serum human TNF-α concentrations[5]. CGS 21680 (0.1mg/kg) was intraperitoneally injected into mice with pleurisy, which significantly reduced the levels of inflammatory factors, neutrophil infiltration and the extent of lung injury[6]. CGS 21680 (0.1mg/kg) was intraperitoneally injected into mice with spinal cord injury, which reduced tissue damage, influx of myeloperoxidase-positive leukocytes, nuclear factor-κB activation and iNOS expression in spinal cord tissue, and reduced JNK MAPK activation in spinal cord oligodendrocytes[7].
References:
[1] Varani K, Gessi S, Merighi S, et al. Adenosine A2A receptors of human circulating blood elements[J]. Drug development research, 1998, 45(3‐4): 253-260.
[2] O'regan M H, Simpson R E, Perkins L M, et al. The selective A2 adenosine receptor agonist CGS 21680 enhances excitatory transmitter amino acid release from the ischemic rat cerebral cortex[J]. Neuroscience letters, 1992, 138(1): 169-172.
[3] Anderson R, Visser S S, Ramafi G, et al. Accelerated resequestration of cytosolic calcium and suppression of the pro‐inflammatory activities of human neutrophils by CGS 21680 in vitro[J]. British journal of pharmacology, 2000, 130(4): 717-724.
[4] Säve S, Mohlin C, Vumma R, et al. Activation of adenosine A2A receptors inhibits neutrophil transuroepithelial migration[J]. Infection and immunity, 2011, 79(8): 3431-3437.
[5] Geraghty N J, Adhikary S R, Watson D, et al. The A2A receptor agonist CGS 21680 has beneficial and adverse effects on disease development in a humanised mouse model of graft-versus-host disease[J]. International Immunopharmacology, 2019, 72: 479-486.
[6] Impellizzeri D, Di Paola R, Esposito E, et al. CGS 21680, an agonist of the adenosine (A2A) receptor, decreases acute lung inflammation[J]. European journal of pharmacology, 2011, 668(1-2): 305-316.
[7] Genovese T, Melani A, Esposito E, et al. The selective adenosine A2A receptor agonist CGS 21680 reduces JNK MAPK activation in oligodendrocytes in injured spinal cord[J]. Shock, 2009, 32(6): 578-585.
| Cell experiment [1]: | |
Cell lines | UROtsa cells、human neutrophils |
Preparation Method | Serum-free culture medium (without penicillin and streptomycin) containing 108 CFU/ml of UPEC strain IA2 was added to the bottom well of transwell inserts for 24h. Bacterial multiplication was limited by incubating the UROtsa cells with gentamicin (50μg/mL) 24h prior to infection. Human neutrophils were prepared as described above, and 3×106 neutrophils were added to the top well. Samples were taken from the bottom well after 0, 1, 2, and 3h. The number of neutrophils that had migrated was counted in a Bürker chamber. To examine the role of adenosine receptor activation in transuroepithelial neutrophil migration, adenosine (10μM) or the specific A2A receptor agonist CGS 21680 (1μM) was added to the top well together with neutrophils after 24h of UPEC infection. |
Reaction Conditions | 1µM; 3h |
Applications | When cells were stimulated with the A2A receptor agonist CGS 21680, UPEC-evoked migration was significantly decreased after 1h and 2h. |
| Animal experiment [2]: | |
Animal models | NSG mice |
Preparation Method | Female NSG mice aged 6–8 weeks were injected i.p. daily (day 2 to day 11) with saline/0.2% DMSO (vehicle) or vehicle containing CGS 21680 (0.1mg/kg). hPBMCs, isolated by density centrifuga tion using Ficoll-Paque PLUS and resuspended in Dulbecco's phosphate-buffer saline , were injected i.p. (day 0) (10×106 hPBMCs/mouse). At 3 weeks post-hPBMC injection, mice were checked for en graftment by immunophenotyping of tail vein blood. Mice were monitored for signs of GVHD using a scoring system, giving a total clinical score out of 10. Mice were euthanized at 10weeks post-injection of hPBMCs, or earlier if exhibiting a clinical score of ≥8 or a weight loss of ≥10%, according to the approved animal ethics protocol. |
Dosage form | 0.1mg/kg; i.p. |
Applications | CGS 21680 increased weight loss, and failed to reduce the clinical score or increase survival in this humanised mouse model of GVHD. CGS 21680 reduced T regulatory cells and increased serum human IL-6 concentrations. CGS 21680 reduced serum human tumor necrosis factor (TNF)-α concentrations and leukocyte infiltration into the liver. |
References: | |
| Cas No. | 120225-54-9 | SDF | |
| Chemical Name | 3-[4-[2-[[6-amino-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]purin-2-yl]amino]ethyl]phenyl]propanoic acid | ||
| Canonical SMILES | CCNC(=O)C1C(C(C(O1)N2C=NC3=C2N=C(N=C3N)NCCC4=CC=C(C=C4)CCC(=O)O)O)O | ||
| Formula | C23H29N7O6 | M.Wt | 499.52 |
| Solubility | ≥ 19.25mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0019 mL | 10.0096 mL | 20.0192 mL |
| 5 mM | 0.4004 mL | 2.0019 mL | 4.0038 mL |
| 10 mM | 0.2002 mL | 1.001 mL | 2.0019 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *