MRS4719
MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.
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- CAS No.: 2840581-32-8
- Formule: C26H13N5O3S.C6H15N
- Masse moléculaire:504.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
IC50: 0.503 μM (P2X4 receptor)[1]
In Vitro
MRS4719 (compound 21u) (0.1, 0.3, 0.6, 1.0 and 3.0 μM; 15 min) inhibits P2X4R-mediated Ca2+ influx in primary human monocyte-derived macrophages.[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female young C57B/6 mice (8-12 weeks; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)[1]
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Dosage:0.5, 1.5 and 3 mg/kg
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Administration:3 days continuous infusion with an Alzet minipump
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Result:Caused significant neuroprotection using total hemispheric infarct volume size at doses 1.5 and 3.0 mg/kg.
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Animal Model:Middle-aged C57B/6 mice (11-12 month-old; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)[1]
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Dosage:1.5 and 3 mg/kg
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Administration:3 days continuous infusion with an Alzet minipump
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Result:Did not improve motor coordination and balance as assessed using rotarod.
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Animal Model:Middle-aged C57B/6 mice (11-12 month-old; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)[1]
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Dosage:3 mg/kg
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Administration:3 days continuous infusion with an Alzet minipump
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Result:Improved dose-dependently learning and memory after stroke and reached statistical significance at a dose of 3 mg/kg.
Chemical Information
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CAS No. 2840581-32-8
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Masse moléculaire 504.60
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Formule C26H13N5O3S.C6H15N
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SMILES
CC[NH+](CC)CC.O=C(NC1=C2C=CC=CC2=CC=C1N3C4=CC(C([N-]5)=NOC5=S)=NC=C4)CC3=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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRS4719 Related Classifications
HY-151547 Related Classifications
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