1377273-00-1
1377273-00-1 structure
- Name: MRS 5698
- Chemical Name: mrs5698
- CAS Number: 1377273-00-1
- Molecular Formula: C28H23ClF2N6O3
- Molecular Weight: 564.97000
- Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
- Create Date: 2018-01-20 06:44:52
- Modify Date: 2024-09-12 09:42:54
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MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis[1][2].
| Name | mrs5698 |
|---|---|
| Synonyms |
(1S,2R,3S,4R,5S)-4-(6-(3-chlorobenzylamino)-2-((3,4-difluorophenyl)ethynyl)-9H-purin-9-yl)-2,3-dihydroxy-N-methylbicyclo[3.1.0]hexane-1-carboxamide
2-(3,4-difluorophenylethynyl)-N6-(3-chlorobenzyl)-(N)-methanocarbaadenosine-5'-methyluronamide |
| Description | MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis[1][2]. |
|---|---|
| Related Catalog | |
| Target |
Adenosine A3 receptor:~3 nM (Ki) |
| In Vitro | MRS5698 displays higher affinity and selectivity (>3000-fold) agonist A3R vs. other adenosine receptor (ARs) in both human and mouse[1]. MRS5698 (0.1-10 µM; 1 hours) induces a concentration-dependently robust A3R-mediated cAMP reduction in HEK-293T cells permanently expressing the A3R, regardless the illumination condition[3]. |
| In Vivo | MRS5698 (3 nmol/day; intrathecal injection for 25 days) prevents Oxaliplatin-induced mechano-allodynia and hyperalgesia, and attenuates Oxaliplatin-induced NLRP3/IL-1β neuroinflammation[2]. MRS5698 (1 mg/kg; i.p. at days 2, 3 ) reduces the IL-23 induced (IL23 injected in day 0, 1, 3) ear thickness of C57BL/6N mouse during the third and fourth experimental days[3]. Animal Model: Oxaliplatin-induced Male Sprague Dawley rats (200–250 g starting weight)[2] Dosage: 3 nmol/day Administration: Intrathecal injection for 25 days Result: Increased the value of mechanical paw withdrawal threshold in grams (PWT) in rat. Attenuated oxaliplatin-induced expression of NLRP3 and maturation of caspase 1 in the DH-SC. Reduced IL-1β levels in the spinal cord. |
| References |
| Molecular Formula | C28H23ClF2N6O3 |
|---|---|
| Molecular Weight | 564.97000 |
| Exact Mass | 564.14900 |
| PSA | 125.19000 |
| LogP | 3.26250 |