2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor Sigma Receptor
  4. EST73502

EST73502 是一种选择性的，具有口服活性的，可透过血脑屏障的 μ-opioid 受体 (μ-opioid receptor/MOR) 激动剂和 σ1 受体(σ1R) 拮抗剂，对 MOR 和 σ1R 作用的 Ki 值分别为 64 nM 和 118 nM。EST73502 可用于缓解疼痛研究。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 EST73502 monohydrochloride 通常具有更好的水溶性和稳定性。

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EST73502 Chemical Structure

EST73502 Chemical Structure

CAS No. : 1838622-25-5

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EST73502 的其他形式现货产品:

Customer Review

Other Forms of EST73502:

EST73502 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 Sigma Receptor 亚型特异性产品:

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Sigma 1 Receptor Sigma 2 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity[1].

IC50 & Target

Ki: 64 nM (MOR), 118 nM (σ1R)[1]
体内研究
(In Vivo)

EST73502 (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC50 of 14 mg/kg in the paw pressure test in CD1 male mice[1].
EST73502 (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice[1].

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

Animal Model: Male CD1 mice, PSNL model[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, twice a day, for 10 days
Result: Attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%.
分子量

352.42

Formula

C19H26F2N2O2
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

EST73502 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

EST735021838622-25-5EST 73502EST-73502Opioid ReceptorSigma ReceptoranalgesicacutechronicpainantinociceptionInhibitorinhibitorinhibit

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目录号：
HY-134189
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