1. TGF-beta/Smad
  2. TGF-β Receptor
  3. THRX-144644

THRX-144644 是一种肺限制性 ALK5 抑制剂,其 IC50 值为 0.14 nM。THRX-144644 避免了与 TGFβ 途径抑制相关的全身毒性。

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THRX-144644 Chemical Structure

THRX-144644 Chemical Structure

CAS No. : 2442519-59-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition[1].

IC50 & Target[1]

ALK5

0.14 nM (IC50)

体外研究
(In Vitro)

THRX-144644 (1-10000 nM; 1 h) inhibits ALK5 with an IC50 value of 23 nM in human BEAS2B cell line.

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

体内研究
(In Vivo)

THRX-144644 (2-60 mg/kg; Inhalation: nebulizer, daily, for 14 days) is a Lung-selective inhibitor and targets to the lungs in Sprague Dawley rats[1].

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

Animal Model: Sprague Dawley rats[1]
Dosage: 2, 10, and 60 mg/kg
Administration: Inhalation: nebulizer, daily, for 14 days
Result: Had the L:P ratio (AUC) was 0.44.
Had lung-to-plasma ratios ranged from 100- to 1200-fold in rats across dose level.
Had lung trough (24 h) concentrations in rats ranged from 3- to 17-fold above the PCLS IC50 across tolerated doses.
分子量

512.00

Formula

C26H28ClF2N7

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

THRX-144644 相关分类

  • 摩尔计算器

  • 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:
THRX-144644
目录号:
HY-150169
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