MRS 1220
Modify Date: 2024-01-02 12:46:42
MRS 1220 structure
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Common Name | MRS 1220 | ||
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| CAS Number | 183721-15-5 | Molecular Weight | 403.82 | |
| Density | 1.49g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C21H14ClN5O2 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of MRS 1220MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2]. |
| Name | N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide |
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| Synonym | More Synonyms |
| Description | MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2]. |
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| Related Catalog | |
| In Vitro | MRS 1220 reverses the effect of A3 agonist-elicited inhibition of tumor necrosis factor-α formation in the human macrophage U-937 cell line with an IC50 of 0.3 μM[1]. VEGF secretion in U87MG glioblastoma stem-like cells (GSCs) decreases ~25% with MRS1220 after 72 h of hypoxia[2]. Cell Viability Assay[2] Cell Line: U87MG GSCs Concentration: 10 μM Incubation Time: 72 hours Result: Decreased ~25% VEGF secretion. |
| In Vivo | MRS1220 (0.15 mg/kg; intraperitoneal inoculation) reduces tumor size and blood vessel formation in vivo. MRS1220 exhibits a strong in vivo anti-angiogenic effect[2]. Animal Model: Eight, 8 week-old male Sprague-Dawley rats bearing C6 (GSCs)[2] Dosage: 0.15 mg/kg/72 h Administration: Administered by intraperitoneal inoculation, for fifteen days Result: A reduction close to 80% and 90% in tumor volume compared to the vehicle-treated group at day ten and fifteen post-treatment, respectively. |
| References |
| Density | 1.49g/cm3 |
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| Molecular Formula | C21H14ClN5O2 |
| Molecular Weight | 403.82 |
| Exact Mass | 403.08400 |
| PSA | 85.32000 |
| LogP | 4.44510 |
| Index of Refraction | 1.744 |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
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Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models.
J. Med. Chem. 58 , 9578-90, (2015) Fragment-based lead discovery (FBLD) holds great promise for drug discovery, but applications to G protein-coupled receptors (GPCRs) have been limited by a lack of sensitive screening techniques and s... |
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Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
J. Med. Chem. 39 , 4142-4148, (1996) The adenosine antagonist 9-chloro-2-(2-furanyl)[1,2,4]triazolo[1,5-c]quinazolin-5-amine (CGS15943) binds to human A3 receptors with high affinity (Ki = 14 nM), while it lacks affinity at rat A3 recept... |
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Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.
Neuropharmacology 36 , 1157-1165, (1997) The effects of putative A3 adenosine receptor antagonists of three diverse chemical classes (the flavonoid MRS 1067, the 6-phenyl-1,4-dihydropyridines MRS 1097 and MRS 1191, and the triazoloquinazolin... |
| MRS 1220 |
| 9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline |
| Tocris-1217 |
| MFCD01321046 |