183721-15-5
183721-15-5 structure
- Name: MRS 1220
- Chemical Name: N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide
- CAS Number: 183721-15-5
- Molecular Formula: C21H14ClN5O2
- Molecular Weight: 403.82
- Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
- Create Date: 2018-12-21 21:46:53
- Modify Date: 2024-01-02 12:46:42
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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].
| Name | N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide |
|---|---|
| Synonyms |
MRS 1220
9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline Tocris-1217 MFCD01321046 |
| 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 |
|---|---|
| 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 |