2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor Arrestin
  4. MP1202

MP1202 是一种 MOR 和 KOR 的双功能激动剂，对 mMOR-1 和 mKOR-1 的 EC50 分别为 0.32 μM 和 0.13 μM。MP1202 具有功能选择性，可减少 hMOR 和 hKOR 中 β-arrestin1/2 募集但显著激活 G 蛋白和 Gα 亚型。MP1202 在亚型选择性阿片类药物敲除小鼠模型中表现出强效的抗伤害作用，且无典型的阿片类药物副作用，但出现条件性位置偏爱和厌恶行为，具有镇痛研究潜力。

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MP1202

MP1202 Chemical Structure

CAS No. : 2578974-82-8

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MP1202 相关抗体

Top Publications Citing Use of Products

查看 Opioid Receptor 亚型特异性产品:

查看所有亚型
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

查看 Arrestin 亚型特异性产品:

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Arrestin-2/β-Arrestin 1 Arrestin-3/β-Arrestin 2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MP1202 is a dual-functional agonist of MOR and KOR with EC50s of 0.32 and 0.13  μM for mMOR-1 and mKOR-1, respectively. MP1202 has functional selectivity with reduction of β-arrestin1/2 recruitment but significant activation of G-protein and Gα-subtype at hMOR and hKOR. MP1202 has potent antinociceptive effects without typical opioid side effects, but it shows conditioned place preference and aversion behaviors in subtype-selective opioid KO mice model, promising for analgesia research[1].

IC50 & Target[1]

Arrestin-2/β-Arrestin 1

 

μ Opioid Receptor/MOR

0.32 μM (EC50)

κ Opioid Receptor/KOR

0.13 μM (EC50)

分子量

556.44

Formula

C27H29IN2O3
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

MP1202 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MP12022578974-82-8MP 1202MP-1202Opioid ReceptorArrestinDual-functional agonistAntinociceptiveβ-arrestin1/2G-proteinSubtype-selective opioid KO mice modelCHO cellsAnalgesiaInhibitorinhibitorinhibit

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目录号：
HY-175197
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