2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. PIPE-3297

PIPE-3297 (compound 25) 是一种选择性的 kappa 阿片受体 (KOR) 激动剂，可以激活 G 蛋白信号通路，EC50 为 1.1 nM，并表现出低 β-arrestin-2 招募活性 (10%)。PIPE-3297 诱导髓鞘形成并具有抗炎作用。

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PIPE-3297 Chemical Structure

PIPE-3297 Chemical Structure

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2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
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Customer Review

PIPE-3297 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity[1].

IC50 & Target

κ Opioid Receptor/KOR

1.1 nM (EC50)

体外研究
(In Vitro)

PIPE-3297 (0.5-1 μM) 诱导髓鞘形成并导致少突胶质祖细胞 (OPC) 分化为少突胶质细胞 (OL)[1].
PIPE-3297 具有心脏毒性，会对 hERG 钾离子通道形成抑制，抑制效率为 72% (3 μM)，并且在肝微粒体中展现出不稳定性[1]。

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

PIPE-3297 相关抗体:

Immunofluorescence[1]

Cell Line: OPC
Concentration: 0.5-1 μM
Incubation Time: 72 h
Result: Increased levels of MBPs
体内研究
(In Vivo)

PIPE-3297 (30 mg/kg，皮下注射，单剂量) 使 CNS 中 KOR 的占有量达到 90%，在大脑中浓度达到 12.5 μM。在 C57BL/6 小鼠 中没有发现 KOR 介导的运动不足的证据[1]。
PIPE-3297 (30 mg/kg，皮下注射，单剂量) 在 C57BL/6 小鼠中诱导 KOR 依赖的 OPC 分化为成熟 OL 细胞[1]。
PIPE-3297 (3 和 30 mg/kg，皮下注射，23 天) 改善 C57BL/6 小鼠髓磷脂少突胶质细胞糖蛋白 (MOG) 诱导的自身免疫性脑脊髓炎 (EAE)[1]。

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

Animal Model: MOG induced EAE in C57BL/6 mice[1]
Dosage: 3 and 30 mg/kg
Administration: s.c., daily for 23 days
Result: Ameliorated the EAE.
Animal Model: C57BL/6 mice[1]
Dosage: 3 and 30 mg/kg
Administration: s.c., single dose
Result: Increased levels of KOR and mature OLs, maintained the locomotion ability.
分子量

350.50

Formula

C23H30N2O
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

PIPE-3297 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:

PIPE-3297PIPE3297PIPE 3297Opioid ReceptorKORβ-arrestin-2 recruitmentmyelinationautoimmune encephalomyelitisOPCOLInhibitorinhibitorinhibit

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产品名称：
PIPE-3297
目录号：
HY-163277
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