MRS7469
MRS7469 is a highly selective A1 adenosine receptor (A1AR) agonist with over 2000-fold selectivity over other adenosine receptor subtypes. MRS7469 stably binds to the orthosteric binding site of A1AR, and exhibits extremely high affinity for both humans and mice (e.g., human pKi is 8.67, mouse pKi is 9.43). By activating central A1AR, MRS7469 significantly induces hypothermia, motor inhibition and psychomotor dysfunction, and can be widely used in research related to depression and other relevant fields.
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- No. CAS: 2257428-48-9
- Fòrmula: C21H28ClN5O3
- Peso molecular:433.93
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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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hA1AR 2.14 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero 76 | CC50 |
28 μM
Compound: 30
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Cytotoxicity against monkey Vero 76 cells by neutral red uptake assay
Cytotoxicity against monkey Vero 76 cells by neutral red uptake assay
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[PMID: 33031923] |
MRS7469 exhibits high binding affinity for hA1AR (pKi=8.67) and mA1AR (pKi=9.43), while its affinity for hA2AAR, hA3AR and mA3AR is much lower[2].
MRS7469 exhibits a binding affinity of 2.14 nM for targeting hA1AR, with over 2000-fold selectivity over other adenosine receptor subtypes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[2]
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Dosage:52 µg/kg (i.c.v.)
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Administration:i.c.v.
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Result:Induced intense hypothermia.
Activated central A1 adenosine receptors preferentially over peripheral A3 adenosine receptors, leading to A1 adenosine receptor-dependent hypothermia and locomotor depression.
Exhibited a high affinity for mouse A1 adenosine receptors (Ki=0.37 nM).
Crossed the blood-brain barrier sufficiently to activate central A1 adenosine receptors.
Chemical Information
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No. CAS 2257428-48-9
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Peso molecular 433.93
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Fòrmula C21H28ClN5O3
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SMILES
OC[C@]12[C@]([C@@H](N3C4=NC(Cl)=NC(NC(C5CCC5)C6CCC6)=C4N=C3)[C@@H]([C@@H]2O)O)([H])C1
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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
[2]. Jacobson KA, et al. Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development. Front Cell Neurosci. 2019;13:124. Published 2019 Mar 28. [Content Brief]
[3]. Salmaso V, et al. In Silico Drug Design for Purinergic GPCRs: Overview on Molecular Dynamics Applied to Adenosine and P2Y Receptors. Biomolecules. 2020;10(6):812. Published 2020 May 26. [Content Brief]
[4]. Oliva P, et al. 2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A1 Adenosine Receptor Positive Allosteric Modulators. ACS Med Chem Lett. 2023;14(12):1640-1646. Published 2023 Nov 13. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRS7469 Related Classifications
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