MRS2339
MRS2339 is a ribose-modified nucleotide and a nucleotidase-resistant P2 receptor agonist. MRS2339 activates P2X4R. MRS2339 induces ionic currents via P2X receptors, reduces cardiomyocyte cross-sectional area and heart weight/body weight ratio, lacks vasodilatory activity, and extends the lifespan of mice with cardiomyopathy. MRS2339 can be used in research related to heart failure and cardiomyopathy.
For research use only. We do not sell to patients.
- CAS No.: 436847-13-1
- Formula: C12H15ClN5O6P
- Molecular Weight:391.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All P2X Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
P2X4 Receptor |
In Vitro
MRS2339 (10 μM) induces a P2X-like ionic current with identical voltage dependence and reversal potential to 2-meSATP in isolated wild-type and CSQ mouse ventricular cardiac myocytes[1].
MRS2339 (10-9-10-5 M) shows no vasodilator effect in isolated wild-type mouse thoracic aorta ring preparations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:calsequestrin (CSQ) transgenic (TG) mice (either sex, ~3 months old)[1]
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Dosage:3 μM
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Administration:miniosmotic pump; ~6 μl/day; 28 days
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Result:Increased median lifespan to 115 days (log rank test, P = 0.02) compared to vehicle controls.
Reduced cardiac myocyte cross-sectional area to 281 μm2 (n = 6 mice, P < 0.05 vs.
vehicle).
Reduced heart weight-to-body weight ratio to 10.5 mg/gram (n = 9 hearts, P < 0.05 vs.
vehicle).
Chemical Information
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CAS No. 436847-13-1
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Molecular Weight 391.70
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Formula C12H15ClN5O6P
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SMILES
OP(OC[C@]12[C@H]([C@@H](O)[C@H](N3C4=NC(Cl)=NC(N)=C4N=C3)[C@H]1C2)O)(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Purity & Documentation
References
[1]. Shen JB, et al. P2X purinergic receptor-mediated ionic current in cardiac myocytes of calsequestrin model of cardiomyopathy: implications for the treatment of heart failure. Am J Physiol Heart Circ Physiol. 2007;292(2):H1077-H1084. [Content Brief]
[2]. Shen JB, et al. Prevention and rescue of cardiac dysfunction by methanocarba adenosine monophosphonate derivatives. Purinergic Signal. 2020;16(1):61-72. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRS2339 Related Classifications
HY-182642 Related Classifications
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Keywords
- MRS2339
- 436847-13-1
- MRS 2339
- MRS-2339
- P2X Receptor
- Nucleoside Antimetabolite/Analog
- cardiomyopathic mice
- heart failure
- cardiac hypertrophy
- cardiomyopathy
- cardiac myocytes
- wild-type mouse thoracic aorta ring preparations
- CSQ mice
- P2X4 receptors
- CSQ mouse ventricular cardiac myocytes
- P2X receptors
- Inhibitor
- inhibitor
- inhibit