1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. PF-03246799

PF-03246799  (Synonyms: 化合物 T24627)

目录号: HY-119103
产品使用指南

PF-03246799 (PF-3246799) 是一种有效的选择性 5-HT2C 受体激动剂,EC50 为 190 nM,Ki 为 160 nM。PF-03246799 显示对 5-HT2C 的选择性高于 5-HT2A 和 5-HT2B 受体。PF-03246799 具有用于压力性尿失禁 (SUI) 研究的潜力。

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PF-03246799 Chemical Structure

PF-03246799 Chemical Structure

CAS No. : 1065110-62-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-03246799 (PF-3246799) is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research[1].

IC50 & Target[1]

5-HT2C Receptor

190 nM (EC50)

5-HT2C Receptor

160 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 EC50
4.5 nM
Compound: 7b, PF-3246799
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
[PMID: 21195614]
NIH3T3 EC50
190 nM
Compound: 7b, PF-3246799
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay
[PMID: 21195614]
NIH3T3 EC50
4.5 nM
Compound: 7b, PF-3246799
Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
[PMID: 21195614]
NIH3T3 EC50
68 nM
Compound: 7b, PF-3246799
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
[PMID: 21195614]
分子量

239.32

Formula

C15H17N3

CAS 号
中文名称

化合物 T24627

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)

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.

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产品名称:
PF-03246799
目录号:
HY-119103
需求量: