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MRS1220, a selective and potent antagonist for the human A3 adenosine receptor (hA3AR) with a dissociation constant (Ki) of 0.59 nM, exhibits therapeutic promise for central nervous system disease research. It effectively diminishes glioblastoma tumor size and inhibits blood vessel formation in vivo.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 42 € | In Stock | |
5 mg | 112 € | In Stock | |
10 mg | 177 € | In Stock | |
25 mg | 303 € | In Stock | |
50 mg | 437 € | In Stock | |
100 mg | 615 € | In Stock | |
500 mg | Inquiry | In Stock |
Description | MRS1220, a selective and potent antagonist for the human A3 adenosine receptor (hA3AR) with a dissociation constant (Ki) of 0.59 nM, exhibits therapeutic promise for central nervous system disease research. It effectively diminishes glioblastoma tumor size and inhibits blood vessel formation in vivo. |
In vitro | MRS 1220 reverses the A3 agonist-induced inhibition of tumor necrosis factor-α formation in the human macrophage U-937 cell line with an IC50 of 0.3 μM[1], and decreases VEGF secretion by approximately 25% in U87MG glioblastoma stem-like cells (GSCs) after 72 hours of hypoxia[2]. |
In vivo | MRS1220 (0.15 mg/kg; intraperitoneal inoculation) significantly reduces tumor size and blood vessel formation in vivo, exhibiting a strong anti-angiogenic effect[2]. |
Alias | MRS 1220 |
Molecular Weight | 403.82 |
Formula | C21H14ClN5O2 |
Cas No. | 183721-15-5 |
Smiles | Clc1ccc2nc(NC(=O)Cc3ccccc3)n3nc(nc3c2c1)-c1ccco1 |
Relative Density. | 1.49 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO: <1 mg/mL (insoluble or slightly soluble) |
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