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100mg | ||
250mg | ||
500mg |
ln Vitro |
CGS21680 markedly increased the expression of CD39 and CD73. Adenosine triphosphate (ATP) hydrolysis and adenosine synthesis are accelerated by CGS21680 [1]. While CGS21680 (10 nM) by itself demonstrated very little survival activity, the addition of the phosphodiesterase inhibitor IBMX greatly increased this activity. Neurotrophin receptor transactivation and the adenylyl cyclase-cAMP-PKA pathway work together to provide CGS21680's survival effect on cultured motor neurons [4].
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ln Vivo |
The intervention CGS21680 (1 mg/kg/ip) encourages the growth of EAN. In Lewis rats, CGS21680 aggravates experimental autoimmune neuritis brought on by bovine peripheral myelin. A drop in CD4+ Foxp3+ T cells and an increase in CD4+ CXCR5+ T cells, B cells, dendritic cells, and antigen-specific autoantibodies are observed in conjunction with the worsening of the disease; the latter may be brought on by CGS21680-induced IL-2 suppression [2]. Rats treated with CGS21680 (0.1 mg/kg, i.p.) saw a brief rise in heart rate but no change in blood pressure; at 0.01 mg/kg, neither the heart rate nor blood pressure changed. Both dosages of CGS21680 prevented cerebral impairments from the first day to seven days following acute MCAo. During this period, it enhanced the cellularity of the ischemic cortex and striatum, decreased microgliosis and astrogliosis, and improved myelin structure in the striatum. CGS21680 decreased the amount of granulocytes infiltrating into ischemic tissue two days following transient MCAo [3].
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References |
[1]. Bao R, et al. Adenosine and the adenosine A2A receptor agonist, CGS21680, upregulate CD39 and CD73 expression through E2F-1 and CREB in regulatory T cells isolated from septic mice. Int J Mol Med. 2016 Sep;38(3):969-75.
[2]. Rosaria Volpini, et al. Adenosine receptor agonists: synthesis and binding affinity of 2-(aryl)alkylthioadenosine derivatives. [3]. Zhang M, et al. Activation of the adenosine A2A receptor exacerbates experimental autoimmune neuritis in Lewis rats in association with enhanced humoral immunity. J Neuroimmunol. 2016 Apr 15;293:129-36. [4]. Melani A, et al. Low doses of the selective adenosine A2A receptor agonist CGS21680 are protective in a rat model of transient cerebral ischemia. Brain Res. 2014 Mar 10;1551:59-72. [5]. Komaki S, et al. Trk and cAMP-dependent survival activity of adenosine A(2A) agonist CGS21680 on rat motoneurons in culture. Neurosci Lett. 2012 Jul 26;522(1):21-4 |
Molecular Formula |
C23H29N7O6
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Molecular Weight |
499.5197
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CAS # |
120225-54-9
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Related CAS # |
CGS 21680 Hydrochloride;124431-80-7
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SMILES |
O1[C@]([H])(C(N([H])C([H])([H])C([H])([H])[H])=O)[C@]([H])([C@]([H])([C@]1([H])N1C([H])=NC2=C(N([H])[H])N=C(N([H])C([H])([H])C([H])([H])C3C([H])=C([H])C(=C([H])C=3[H])C([H])([H])C([H])([H])C(=O)O[H])N=C12)O[H])O[H]
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 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 | 1.0010 mL | 2.0019 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.