1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. ASP7657 free base

ASP7657 free base 是一种具有口服活性的 EP4 受体 拮抗剂,对人和大鼠 EP4 受体的 Ki 分别为 2.21 和 6.02 nM。

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ASP7657 free base Chemical Structure

ASP7657 free base Chemical Structure

CAS No. : 1196045-28-9

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1 mg ¥1422
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ASP7657 free base is an orally active EP4 receptor antagonist, with Kis of 2.21 and 6.02 nM for the human and rat EP4 receptors[1].

IC50 & Target[1]

hEP4

2.21 nM (IC50)

rat EP4

6.02 nM (IC50)

体外研究
(In Vitro)

ASP7657 free base 抑制 CHO 细胞 (表达 EP4 受体) 和人淋巴母细胞样 T 细胞中 PGE2 诱导的 cAMP 增加,IC50 值分别为 0.86 nM、0.29 nM[1]

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

体内研究
(In Vivo)

ASP7657 (0.1 mg/kg,口服,大鼠) 显示出 t1/2 为 1.38 h,Cmax 为 22.4 ng/mL,口服生物利用度为 46.2%[1].
ASP7657 (0.003-0.1 mg/kg,口服) 抑制 LPS (1 μg/mL) 诱导的大鼠的全血中 TNF-α 释放[1]
ASP7657 (0.01 mg/kg,口服) 减少 2 型糖尿病小鼠中的尿白蛋白排泄[1]

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

Animal Model: LPS (1 μg/mL)-induced rats[1]
Dosage: 0.003, 0.01, 0.03, 0.1 mg/kg
Administration: p.o.
Result: Antagonized the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, in a dose-dependent way.
Clinical Trial
分子量

509.52

Formula

C28H26F3N3O3

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

ASP7657 free base 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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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)
× = ×
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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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ASP7657 free base
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HY-120598
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