2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. 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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MRS4719

MRS4719 構造式

CAS 番号 : 2840581-32-8

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MRS4719 関連抗体

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製品説明

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[1].

IC50 & Target

IC50: 0.503 μM (P2X4 receptor)[1]
体外実験

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.

MRS4719 関連抗体
体内実験

MRS4719 (compound 21u) (0.5-3 mg/kg; 3 days continuous infusion with an Alzet minipump) reduce infarct volume and reduced brain atrophy; does not improve motor coordination and balance as assessed using rotarod; improves learning and memory after stroke[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 0.5, 1.5 and 3 mg/kg
Administration: 3 days continuous infusion with an Alzet minipump
Result: Caused significant neuroprotection using total hemispheric infarct volume size at doses 1.5 and 3.0 mg/kg.
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]
Dosage: 1.5 and 3 mg/kg
Administration: 3 days continuous infusion with an Alzet minipump
Result: Did not improve motor coordination and balance as assessed using rotarod.
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]
Dosage: 3 mg/kg
Administration: 3 days continuous infusion with an Alzet minipump
Result: Improved dose-dependently learning and memory after stroke and reached statistical significance at a dose of 3 mg/kg.
分子量

504.60

分子式

C26H13N5O3S.C6H15N
CAS 番号
SMILES

CC[NH+](CC)CC.O=C(NC1=C2C=CC=CC2=CC=C1N3C4=CC(C([N-]5)=NOC5=S)=NC=C4)CC3=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献
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MRS4719 Related Classifications

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Keywords:

MRS47192840581-32-8MRS 4719MRS-4719P2X ReceptorP2XRsInfarctbrain atrophyneuroprotectiveischemic strokemacrophagesoldagingInhibitorinhibitorinhibit

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