SCH 442416Very selective, high affinity A2A antagonist CAS# 316173-57-6 |
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Quality Control & MSDS
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| Cas No. | 316173-57-6 | SDF | Download SDF |
| PubChem ID | 10668061 | Appearance | Powder |
| Formula | C20H19N7O2 | M.Wt | 389.42 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| SMILES | COC1=CC=C(C=C1)CCCN2C3=C(C=N2)C4=NC(=NN4C(=N3)N)C5=CC=CO5 | ||
| Standard InChIKey | AEULVFLPCJOBCE-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C20H19N7O2/c1-28-14-8-6-13(7-9-14)4-2-10-26-18-15(12-22-26)19-23-17(16-5-3-11-29-16)25-27(19)20(21)24-18/h3,5-9,11-12H,2,4,10H2,1H3,(H2,21,24) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). Blocks the cytoprotective effect of A2A agonist CGS-21680. |
SCH 442416 Dilution Calculator
SCH 442416 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5679 mL | 12.8396 mL | 25.6792 mL | 51.3584 mL | 64.198 mL |
| 5 mM | 0.5136 mL | 2.5679 mL | 5.1358 mL | 10.2717 mL | 12.8396 mL |
| 10 mM | 0.2568 mL | 1.284 mL | 2.5679 mL | 5.1358 mL | 6.4198 mL |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5136 mL | 1.0272 mL | 1.284 mL |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.5136 mL | 0.642 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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The effect of A 2A receptor antagonist (SCH 442416) on the mRNA expression of Kir 2.1 and Kir 4.1 channels in rat retinal Muller cells under hypoxic conditions in vitro.[Pubmed:24431311]
Adv Clin Exp Med. 2013 Nov-Dec;22(6):825-9.
OBJECTIVES: To investigate the situation of inwardly rectifying potassium channels Kir 2.1 and Kir 4.1 under hypo-xic conditions, and whether the A2A receptor antagonist could modulate the mRNA expression of Kir 2.1 and Kir 4.1 channels in retinal Muller cells in vitro under hypoxic conditions. MATERIAL AND METHODS: Muller cells were treated with 0.1 1, 10 and 100 microM of A2A receptor antagonist (SCH 442416) under hypoxic conditions for 24 h, and the expression of the Kir 2.1 and Kir 4.1 mRNA channels was examined using real-time polymerase chain reaction (qPCR). RESULTS: There were no significant changes in the mRNA expression of the Kir 2.1 or Kir 4.1 channels under hypoxic conditions compared with normal conditions after 24 h cultured in vitro. The mRNA expression of Kir 2.1 and Kir 4.1 channels treated with 0.1 microM SCH 442416 under hypoxic conditions were increased, but at higher concentrations of SCH 442416, the mRNA expression of the Kir 2.1 and Kir 4.1 channels decreased. CONCLUSIONS: The A2A receptor antagonist (SCH 442416) could increase mRNA expression of the Kir 2.1and Kir 4.1 channels in Muller cells to protect the retinal neurons in vitro under hypoxic conditions.
In vitro effect of adenosine A2A receptor antagonist SCH 442416 on the expression of glutamine synthetase and glutamate aspartate transporter in rat retinal Muller cells at elevated hydrostatic pressure.[Pubmed:22134673]
Oncol Rep. 2012 Mar;27(3):748-52.
The aim of this study was to investigate the effect of an adenosine A2A receptor antagonist on the expression of glutamine synthetase (GS) and glutamate aspartate transporter (GLAST) in rat retinal Muller cells at elevated hydrostatic pressure in vitro. Immunofluorescence staining of GS and GFAP was used for the identification of Muller cells. The expression of GS and GLAST in different hydrostatic pressure (0, 20, 40, 60, 80 mmHg/24 h) was examined by real-time PCR and Western blotting to identify the most suitable pressure. Muller cells treated with 0.1, 1, 10 microM SCH 442416 (A2A receptor antagonist) in the most suitable pressure, and the levels of GS and GLAST were examined by real-time PCR and Western blotting. Significantly increased expression of GS and GLAST at 40 mmHg pressure was observed in Muller cells and treatment with 10 microM SCH 442416 in 40 mmHg pressure further promoted the expression of GS and GLAST. A2A receptor antagonist increased the expression of GLAST and GS of Muller cells and accelerated the clearance of extracellular glutamate.
Effect of A(2A) receptor antagonist (SCH 442416) on the mRNA expression of glutamate aspartate transporter and glutamine synthetase in rat retinal Muller cells under hypoxic conditions in vitro.[Pubmed:22969972]
Exp Ther Med. 2012 May;3(5):803-806.
The purpose of the present study was to investigate the effect of the A(2A) receptor antagonist (SCH 442416) on the mRNA expression of glutamate aspartate transporter (GLAST) and glutamine synthetase (GS) in rat retinal Muller cells under hypoxic conditions in vitro. Immunofluorescent staining of GS and GFAP was used for the identification of Muller cells. The GLAST and GS mRNA expression of Muller cells treated with 0.1, 1 and 10 muM SCH 442416 under hypoxic conditions was examined by real-time PCR. Muller cells increased the mRNA expression of GLAST under hypoxic conditions; those treated with 0.1 muM SCH 442416 showed a further significant increase in the mRNA expression of GLAST in vitro. Although the mRNA expression of GS was decreased under hypoxic conditions, the mRNA expression was increased when Muller cells were treated with 0.1 muM SCH 442416. A(2A) receptor antagonist increased the GLAST and GS expression of Muller cells and accelerated the clearance of extracellular glutamate under hypoxic conditions in vitro.
