| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In HEK293-A2AR cells, A2AR-antagonist-1 (0.001-10 μM; 30 minutes) lowers the levels of phosphorylated ERK generated by NECA [1]. In Jurkat T cells (human immortalized T line), A2AR-antagonist-1 (0.1-10 μM; 5 hours) enhances molecule expression while inhibiting NECA-induced immune molecule expression [1].
A2AR-antagonist-1 (0.1–10 μM; 48 h) improves the activation and activation of external T cells impact function and restores the cytotoxic function damage of OT-I mouse splenocytes (OT-I CTL) to MC38-OVA cells[1]. |
|---|---|
| ln Vivo |
A2AR-antagonist-1 (100 mg/kg; wound cells; once daily for 23 days) showed remarkable anti-tumor effect in the C57BL/6 mouse model with breast cancer MC38 [1]. Metabokinetic analysis[1] Route dose (mg/kg) Cmax (ng/mL) AUC0-last (ng·h/mL) AUC0-t (ng·h/mL) t1/2 (h) F (%) iv 2 2584 5577 5565 0.93 / po 10 8823 24008 24003 2.35 86.1
|
| Cell Assay |
RT-PCR[1]
Cell Types: Jurkat T cells Tested Concentrations: 0.1 μM, 1 μM and 10 μM Incubation Duration: 5 hrs (hours) Experimental Results: Reversal of NECA (1 μM)-induced upregulation of immunosuppressive molecules (LAG-3 and TIM-3) and NECA-induced down-regulation of effector molecules (GZMB, IFNG, and IL-2). Immunofluorescence[1] Cell Types: Cytotoxic T lymphocytes (OT-I CTL) from OT-I mouse splenocytes Tested Concentrations: 0.1 μM, 1 μM and 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: OT-I CTL Relative lethality increases impression. |
| Animal Protocol |
Animal/Disease Models: Mouse MC38 xenograft model [1]
Doses: 100 mg/kg Route of Administration: PO; one time/day for 23 days Experimental Results: Promote CD8+ T cells accumulation. Enhance anti-tumor immunity and promote tumor regression. There was no significant effect on mouse body weight. |
| References |
[1]. Zhu C, et al. Discovery of Pyridinone Derivatives as Potent, Selective, and Orally Bioavailable Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2023 Mar 23.
|
| Molecular Formula |
C27H25N5O2
|
|---|---|
| Molecular Weight |
451.52
|
| CAS # |
2922920-71-4
|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2147 mL | 11.0737 mL | 22.1474 mL | |
| 5 mM | 0.4429 mL | 2.2147 mL | 4.4295 mL | |
| 10 mM | 0.2215 mL | 1.1074 mL | 2.2147 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.
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