2. Cytoskeleton Protein Tyrosine Kinase/RTK
  3. Collagen c-Fms PDGFR Src
  4. Antifibrotic agent 1

Antifibrotic agent 1 是一种口服有效的抗特发性肺纤维化 (IPF) 药物。Antifibrotic agent 1 可有效减弱 IPF 相关过程，包括 TGF-β 诱导的 EMT 和 FMT 过程，以及促纤维化的 M2 极化。Antifibrotic agent 1 选择性抑制 CSF-1R、PDGFR-α 和 Src 家族激酶 (SFKs)，同时不影响 VEGFR、FGFR 和 Abl，以最大限度地减少脱靶毒性。Antifibrotic agent 1 在 Bleomycin (BLM) (HY-108345) 诱导的肺纤维化小鼠模型中具有强效的抗纤维化活性。

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Antifibrotic agent 1 Chemical Structure

Antifibrotic agent 1 Chemical Structure

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Antifibrotic agent 1 相关抗体

Top Publications Citing Use of Products

查看 PDGFR 亚型特异性产品:

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PDGFR PDGFRβ PDGFRα

查看 Src 亚型特异性产品:

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Lck Fyn Blk Hck Lyn Yes SRC-3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model[1].

IC50 & Target[1]

PDGFRα

 

Collagen I

40.5 nM (IC50)

Fyn

 

Hck

 

Lyn

 

Lck

 

Yes

 

体外研究
(In Vitro)

Antifibrotic agent 1 (Compound 22) (0.001-10 μM, 48 h,) 表现出显著的抗纤维化活性，在 1 μM 浓度下可抑制 A549 细胞中 95.0% 的 COL1A1 表达，IC50 为 40.5 nM[1]。
Antifibrotic agent 1 (1-200 μM) 在 A549、HEK293 和 L02 细胞中表现出抗纤维化作用，且细胞毒性较低(CC50 > 200 μM)[1]。
Antifibrotic agent 1 (0.1-10 μM，48 小时) 剂量依赖性地降低 TGF-β 诱导的 A549、HFL1 和 HLFs 细胞的 COL1A1 的蛋白水平，从而抑制 IPF 相关的 EMT 和 FMT 过程[1]。
Antifibrotic agent 1 (1-10 μM，48 小时) 在 10 μM 浓度下可选择性抑制骨髓来源的巨噬细胞 (BMDM) 向促纤维化 M2 表型极化[1]。
Antifibrotic agent 1 (1-100 nM) 可选择性抑制 CSF-1R、PDGFR-α 和 SFKs，从而减轻 IPF 进展，同时保留 VEGFR、FGFR 和 Abl，最大限度地降低脱靶毒性[1]。

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

Antifibrotic agent 1 相关抗体:

Western Blot Analysis[1]

Cell Line: A549 cells, HFL1 cells, HLFs cells
Concentration: 0.1, 0.5, 1, 10 μM
Incubation Time: 48 h after TGF-β stimulated 48 h
Result: Dose-dependently reduced the protein level of COL1A1 in IPF-related EMT and FMT models and primary human lung fibroblasts model.
药代动力学
(Parmacokinetics)
Species Dose SampleTime Route Indicator value
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. T1/2 2.37 hr
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. T1/2 3.15 hr
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. AUClast 437 ng·h/mL
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. Tmax 0.42 hr
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. MRT0-∞ 0.4 hr
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. Cmax 137 ng·h/mL
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. CL 79.8 mL/min/kg
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. MRT0-∞ 2.32 hr
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. Vss 1.802 L/kg
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. F 12.6 %
体内研究
(In Vivo)

Antifibrotic agent 1 (Compound 22) (60 mg/kg，口服，每日一次，共 14 天) 具有中等口服生物利用度和良好的安全性，在 BLM 诱导的肺纤维化小鼠模型中高达 60 mg/kg 的剂量下未见明显的肝毒性或肾毒性[1]。
Antifibrotic agent 1 (60 mg/kg，口服，每日一次，共 10 天) 具有卓越的抗纤维化功效，可显著缓解 BLM 诱导的肺纤维化小鼠模型中的肺纤维化，降低炎症和促纤维化 M2 相关细胞因子水平，并改善肺功能[1]。

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

Animal Model: Male C57BL/6 mice (8 weeks old) were given an intratracheal administration of BLM (1.8 mg/kg) to induce pulmonary fibrosis[1].
Dosage: 30, 60 mg/kg
Administration: Oral gavage (p.o.), daily for 14 days and then measured body and lung tissues weight as well as collected lung tissues.
Result: Significantly alleviated weight losses, increased survival rate and improved lung functions with increased lung coefficient value in mice mode.
Notably downregulated Tgf-β mRNA, reduced both the mRNA and protein levels of Fn1 and Col1a1, and decreased hydroxyproline content in the lung tissues in mice model at the dose of 60 mg/kg.
Significantly reduced Tnf and Ccl2 mRNA levels but increased IL-10 mRNA level, modulating inflammation to further alleviate pulmonary fibrosis in mice model.
Strongly downregulated M2-associated genes (Arg1, Mrc1) but not the M1 marker CD86, selectively inhibiting M2 macrophage polarization without significantly affecting M1 polarization in mice model.
Potently alleviated pathological changes related lung fibrosis and decreased collagen fibers with a 54.6 % reduction in fibrosis area in mice model at the dose of 60 mg/kg.
分子量

498.96

Formula

C27H23ClN6O2
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

Antifibrotic agent 1 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.

Keywords:

Antifibrotic agent 1Antifibrotic agent1Antifibrotic agent-1Collagenc-FmsPDGFRSrcCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RPlatelet-derived growth factor receptorAnti-fibroticIdiopathic pulmonary fibrosisIPFEMTFMTmulti-kinaseBleomycin (BLM)A549 cellsHEK293 cellsL02 cellsInhibitorinhibitorinhibit

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