1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. PF-03382792

PF-03382792 是一种有效的 5-HT4 部分激动剂,对 5-HT4dKi 为 2.7 nM,EC50 为 0.9 nM。PF-03382792 可以透过大脑。PF-03382792 适度增加大鼠前额皮质中的皮质乙酰胆碱。

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PF-03382792 Chemical Structure

PF-03382792 Chemical Structure

CAS No. : 1400811-63-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex[1].

IC50 & Target[1]

5-HT4d Receptor

2.7 nM (Ki)

5-HT4d Receptor

0.9 nM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
0.8 nM
Compound: 3
Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
[PMID: 22974325]
HEK293 EC50
0.9 nM
Compound: 3
Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay
Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay
[PMID: 22974325]
HEK293 EC50
1.15 nM
Compound: 3
Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
[PMID: 22974325]
HEK293 EC50
1.2 nM
Compound: 3
Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
[PMID: 22974325]
HEK293 EC50
1.3 nM
Compound: 3
Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
[PMID: 22974325]
HEK293 EC50
1.52 nM
Compound: 3
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
[PMID: 22974325]
HEK293 EC50
2.15 nM
Compound: 3
Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
[PMID: 22974325]
分子量

433.52

Formula

C23H32FN3O4

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
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  • 稀释计算器

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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:
PF-03382792
目录号:
HY-18138
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