2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. PF-03654764

PF-03654764 是一种具有口服活性的，选择性组胺 H3 受体拮抗剂，对人 H3 和大鼠 H3 的 Ki 值分别为 1.2 nM 和 7.9 nM。PF-03654764 和 Fexofenadine (HY-B0801A) 组合具有用于过敏性鼻炎研究的潜力。

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PF-03654764 Chemical Structure

PF-03654764 Chemical Structure

CAS No. : 935840-35-0

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规格 价格 是否有货 数量
1 mg ￥4000
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Other Forms of PF-03654764:

PF-03654764 相关抗体

Top Publications Citing Use of Products

查看 Histamine Receptor 亚型特异性产品:

查看所有亚型
H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research[1][2].

IC50 & Target[1]

human H3 receptor

1.2 nM (Ki)

rat H3 receptor

7.9 nM (Ki)

human H3 receptor

8.98 (pKi)

rat H3 receptor

8.10 (pKi)

体外研究
(In Vitro)

PF-03654764 has pKi values of 8.98 and 8.10 for human H3 and rat H3 in whole cell assay, respectively. PF-03654764 has pKi values of 8.84, 7.73 and Ki values of 1.4 nM and 19 nM for human H3 and rat H3 in HEK-293 cells, respectively. PF-03654764 has >1000-fold selectivity for the H3 receptor over the other histamine receptor subtypes[1].
PF-03654764 has a human liver microsomes (HLM) T1/2 of 120 min and a HLM CLh <5 mL/min•kg[1].

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

PF-03654764 相关抗体:
体内研究
(In Vivo)

PF-03654764 (10 mL/kg; oral; 14 days) has a Cmax of 8057 ng/mL and an AUC0-24 of 67400 ng•h/mL in Sprague-Dawley rats[1].
PF-03654764 (1 mL/kg; oral; 7 days) has a Cmax of 6302 ng/mL and an AUC0-24 of 18175 ng•h/mL in beagle dogs[1].

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

350.45

Formula

C20H28F2N2O
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

PF-03654764 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:

PF-03654764935840-35-0PF03654764PF 03654764Histamine ReceptororallyH3FexofenadineallergicrhinitisInhibitorinhibitorinhibit

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产品名称：
PF-03654764
目录号：
HY-123812
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