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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- CAS No.: 1377273-00-1
- Formule: C28H23ClF2N6O3
- Masse moléculaire:564.97
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Adenosine A3 receptor ~3 nM (Ki) |
Cellular Effect
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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] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
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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CAS No. 1377273-00-1
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Masse moléculaire 564.97
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Imiquimod-Induced Psoriasiform Dermatitis
Imiquimod (IMQ)-induced psoriasiform dermatitis is a widely used murine model in which topical application of IMQ, a Toll-like receptor 7 (TLR7) agonist, triggers innate immune activation in the skin and induces a psoriasis-like inflammatory cascade characterized by epidermal hyperplasia, immune cell infiltration, and cytokine production dominated by the IL-23/IL-17 axis. This inflammatory response is mediated through activation of dendritic cells and downstream induction of IL-23, IL-17A, IL-22, and related pro-inflammatory mediators, recapitulating key features of human plaque psoriasis and enabling mechanistic and therapeutic studies. The model is commonly induced using Aldara (5% IMQ cream) applied topically to murine skin, resulting in rapid onset of erythema, scaling, and thickening that can be quantified as disease severity indices and validated histologically.
Pureté et documentation
Références
[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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