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

PZ-1657 hydrochloride (Compound 57) 是一种强效,选择性且有口服活性的 5-羟色胺 7 受体 (5-HT7 receptor) 反向激动剂,其 Ki 值为 5 nM。PZ-1657 hydrochloride 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 hydrochloride 能显著降低小鼠海马体中由 5-HT7 受体介导的 MMP-9 活性,其效果与 SB-269970 (HY-15370) 相当。PZ-1657 hydrochloride 可逆转苯环利定 (Phencyclidine) 诱导的大鼠新物体识别实验中观察到的认知缺陷,且不影响动物的自发活动。PZ-1657 hydrochloride 可用于情感障碍的研究,如抑郁症和双相情感障碍。

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PZ-1657 hydrochloride

PZ-1657 hydrochloride Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a Ki of 5 nM. PZ-1657 hydrochloride can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 2.93 nM). PZ-1657 hydrochloride can significantly reduce the MMP-9 activity mediated by 5-HT7 receptors in the hippocampus of mice, and the effect is comparable to that of SB-269970 (HY-15370). PZ-1657 hydrochloride can reverse the cognitive deficits observed in the rat novel object recognition test induced by Phencyclidine without affecting the animals' spontaneous activities. PZ-1657 hydrochloride can be used for the research of emotional disorders, such as depression and bipolar disorder[1].

IC50 & Target[1]

5-HT7 Receptor

5 nM (Ki)

5-HT1A Receptor

292 nM (Ki)

5-HT2A Receptor

435 nM (Ki)

D2 Receptor

1004 nM (Ki)

5-HT6 Receptor

3282 nM (Ki)

MMP-9

 

分子量

495.01

Formula

C23H28ClFN4O3S

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
  • 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)

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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.

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产品名称:
PZ-1657 hydrochloride
目录号:
HY-179724A
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