2. Metabolic Enzyme/Protease MAPK/ERK Pathway Stem Cell/Wnt
  3. Phosphodiesterase (PDE) ERK JNK p38 MAPK
  4. ATX inhibitor 26

ATX inhibitor 26 是一种 Autotaxin (ATX) 抑制剂，在人血浆中的 IC50 为 57 nM。ATX inhibitor 26 可抑制细胞迁移和胶原凝胶收缩。ATX inhibitor 26 具有显著的抗纤维化作用，可减少 Bleomycin (BLM) (HY-108345) 诱导的肺纤维化模型中的胶原沉积。

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ATX inhibitor 26

ATX inhibitor 26 Chemical Structure

CAS No. : 2940248-11-1

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ATX inhibitor 26 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

查看 JNK 亚型特异性产品:

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JNK1 JNK2 JNK3 JNK

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. ATX inhibitor 26 inhibits cell migration and collagen gel contraction. ATX inhibitor 26 has significant anti-fibrotic effects, reducing collagen deposition in a Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis model[1].

IC50 & Target[1]

Autotaxin

57 nM (IC50)

体外研究
(In Vitro)

ATX inhibitor 26 (Compound 27a) (500 nM) 对人血浆中的 ATX (抑制率为 94.1%，IC50：39.2 nM) 和溶血磷脂酶 D (LysoPLD) (抑制率超过 90%，IC50：57.2 nM) 均具有优异的抑制活性[1]。
ATX inhibitor 26 (3.0 μM，12-48 小时) 显著抑制 L132、 A549 和 WI38 细胞中 LPC/TGF-β 诱导的 MAPK 活化[1]。
ATX inhibitor 26 (0-6.0 μM，0.5-6.0 小时) 以剂量和时间依赖性的方式调节 L132 细胞中 MAPK 信号传导，且在 30 分钟内以 ≥0.5 μM 的剂量降低 ERK、p38 和 JNK 的磷酸化水平[1]。
ATX inhibitor 26 (3.0 μM，0-48 小时) 显著降低基底细胞和 TGF-β 诱导的 A549 细胞迁移以及 WI38 细胞的胶原凝胶收缩[1]。

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

ATX inhibitor 26 相关抗体:

Western Blot Analysis[1]

Cell Line: L132 cells
Concentration: 0.1, 0.5, 1.0, 3.0, 6.0 μM
Incubation Time: 0.5, 1.0, 3.0, 6.0 h
Result: Dose- and time-dependently reduced the phosphorylation levels of ERK, p38, and JNK, with effects observed at dose as low as 0.5 μM and within 30 min of treatment.
Significantly suppressed LPC (1 μM) and TGF-β (5 ng/ml)-induced MAPK pathway activation.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 3.0 μM
Incubation Time: 48 h
Result: Significantly reduced both basal and TGF-β-induced migration of epithelial cells.
药代动力学
(Parmacokinetics)
Species Dose SampleTime Route Indicator value
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. Tmax 0.5 hr
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. Cmax 1093.2 μg/mL
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. T1/2 7.5 hr
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. AUClast 3088.3 ng·h/mL
体内研究
(In Vivo)

ATX inhibitor 26 (Compound 27a) (1 或 2 mg/kg，口服，每日一次，持续 21 天) 可减少 BLM 诱导的肺纤维化模型中胶原沉积、LPAR1 和 p-ERK1/2 表达水平，同时降低 α-SMA、Col1A1 和促炎标志物 IL-6、IL-1β 和 INF-γ 的 mRNA 水平[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 BLM (1.8 U/kg/mouse) through intratracheal injection to induce pulmonary fibrosis[1].
Dosage: 1 or 2 mg/kg
Administration: oral gavage (p.o.), once a day for 21 days (7 days prior to BLM administration and 14 days post-BLM), and then collects lung tissue.
Result: Increased survival of BLM-induced pulmonary fibrosis mice.
Significantly reduced collagen deposition, LPAR1, and p-ERK1/2 expression in pulmonary tissue.
Significantly decreased mRNA levels of α-SMA, Col1A1, and pro-inflammatory markers IL-6, IL-1β, and INF-γ in a BLM-induced pulmonary fibrosis model.
Did not induced significant histopathological abnormalities in the liver, kidney, and spleen and notable changes in serum biochemical marker.
分子量

452.29

Formula

C18H19Cl2N7O3
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

ATX inhibitor 26 相关分类

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  • 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:

ATX inhibitor 262940248-11-1ATX inhibitor26ATX inhibitor-26Phosphodiesterase (PDE)ERKJNKp38 MAPKExtracellular signal regulated kinasesc-Jun N-terminal kinaseAutotoxinInhibitorBleomycin (BLM)MAPKFibrosisinhibitorinhibit

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