MRS5698
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.
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- No. CAS: 1377273-00-1
- Fòrmula: C28H23ClF2N6O3
- Peso molecular:564.97
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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Adenosine A3 receptor ~3 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
1.2 nM
Compound: 31, MRS5698
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Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay
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[PMID: 22559880] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Oxaliplatin-induced Male Sprague Dawley rats (200–250 g starting weight)[2]
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Dosage:3 nmol/day
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Administration:Intrathecal injection for 25 days
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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.
Chemical Information
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No. CAS 1377273-00-1
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Peso molecular 564.97
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Fòrmula C28H23ClF2N6O3
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SMILES
CNC([C@]12[C@]([C@](N3C4=NC(C#CC5=CC(F)=C(C=C5)F)=NC(NCC6=CC(Cl)=CC=C6)=C4N=C3)([H])[C@@H]([C@@H]2O)O)([H])C1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Tosh DK, et al. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain. Purinergic Signal. 2015;11(3):371-387. [Content Brief]
[2]. Wahlman C, et al. Chemotherapy-induced pain is promoted by enhanced spinal adenosine kinase levels through astrocyte-dependent mechanisms. Pain. 2018;159(6):1025-1034. [Content Brief]
[3]. López-Cano M, et al. Optical control of adenosine A3 receptor function in psoriasis. Pharmacol Res. 2021 Aug;170:105731. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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