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

MRS4719 是一种有效的 P2X4受体拮抗剂，对人 P2X4 受体的 IC50 为 0.503 μM。MRS4719 可减少脑梗死体积，减少脑萎缩，在缺血性脑中风模型中具有神经保护和神经康复作用。MRS4719 还能减少 ATP 诱导的人单核细胞源性巨噬细胞 [Ca2+]i 内流。MRS4719 可用于研究缺血性脑中风。

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MRS4719 Chemical Structure

MRS4719 Chemical Structure

CAS No. : 2840581-32-8

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MRS4719 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
体外研究
(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 human subjects[1].

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

MRS4719 相关抗体:
体内研究
(In Vivo)

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].

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

Formula

C26H13N5O3S.C6H15N
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MRS4719 相关分类

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Keywords:

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

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