2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. 5-HT Receptor Dopamine Receptor MMP Cytochrome P450
  4. PZ-1657

PZ-1657 (Compound 57) 是一种口服有效、可穿透血脑屏障、选择性高且代谢稳定的 5-HT7 受体 (5-HT7 receptor) 反向激动剂，其 Ki 值为 5 nM。PZ-1657 能够抑制由 Gs 信号通路介导的组成型环磷酸腺苷 (cAMP) 生成 (EC50 值为 2.93 nM)。PZ-1657 可抑制 CYP3A4 P450 (IC50 = 12.2 μM) 和 hERG 通道。PZ-1657 可降低 5-HT7 受体介导的 MMP-9 活性。PZ-1657 逆转 Phencyclidine 诱导的认知功能障碍。PZ-1657 具有抗抑郁特性。

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PZ-1657

PZ-1657 Chemical Structure

1.  客户无需承担相应的运输费用。

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。

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PZ-1657 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

查看 Dopamine Receptor 亚型特异性产品:

查看所有亚型
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

查看 MMP 亚型特异性产品:

查看所有亚型
MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PZ-1657 (Compound 57) is an orally active, blood-brain barrier permeable, highly selective, and metabolically stable 5-HT7 receptor inverse agonist with a Ki value of 5 nM. PZ-1657 inhibits constitutive cyclic adenosine monophosphate (cAMP) production mediated by the Gs signaling pathway (EC50 value of 2.93 nM). PZ-1657 inhibits CYP3A4 P450 (IC50 = 12.2 μM) and hERG channels. PZ-1657 reduces 5-HT7 receptor-mediated MMP-9 activity. PZ-1657 reverses Phencyclidine-induced cognitive impairment. PZ-1657 possesses antidepressant properties[1].

IC50 & Target[1]

MMP-9

 

5-HT7 Receptor

5 nM (Ki)

5-HT1A Receptor

292 nM (Ki)

D2 Receptor

1004 nM (Ki)

CYP3A4

12.2 μM (IC50)

分子量

458.55

Formula

C23H27FN4O3S
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

PZ-1657 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:

PZ-1657PZ1657PZ 16575-HT ReceptorDopamine ReceptorMMPCytochrome P450Serotonin Receptor5-hydroxytryptamine ReceptorMatrix metalloproteinasesCYPscognitive impairmentantidepressantInhibitorinhibitorinhibit

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目录号：
HY-179724
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