2. Metabolic Enzyme/Protease MAPK/ERK Pathway GPCR/G Protein Stem Cell/Wnt
  3. Phosphodiesterase (PDE) p38 MAPK LPL Receptor ERK JNK
  4. Autotaxin-IN-8

Autotaxin-IN-8 (Compound 14E) 是一种具有口服活性 Autotaxin 抑制剂，对 hAutotaxin 的 IC50 为 14.2 nM。Autotaxin-IN-8 抑制 Autotaxin 活性，抑制 MAPK 激活，抑制 LPAR1 和 p-ERK1/2 。Autotaxin-IN-8 降低 JNK、p38 的磷酸化水平。Autotaxin-IN-8 可降低肺纤维化小鼠模型中的胶原沉积。Autotaxin-IN-8 可用于肺纤维化的相关研究。




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Autotaxin-IN-8

Autotaxin-IN-8 Chemical Structure

CAS No. : 3058084-21-9

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Autotaxin-IN-8 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 p38 MAPK 亚型特异性产品:

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

查看 LPL Receptor 亚型特异性产品:

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Autotaxin-IN-8 (Compound 14E) is an orally active Autotaxin inhibitor with an IC50 of 14.2 nM against hAutotaxin. Autotaxin-IN-8 inhibits Autotaxin activity, MAPK activation, LPAR1 and p-ERK1/2. Autotaxin-IN-8 reduces the phosphorylation levels of JNK and p38. Autotaxin-IN-8 decreases collagen deposition in a mouse model of pulmonary fibrosis. Autotaxin-IN-8 can be used in research related to pulmonary fibrosis[1].\n
IC50 & Target[1]

ERK1

 

ERK2

 

LPA1 Receptor

 

体外研究
(In Vitro)

Autotaxin-IN-8 可强效抑制重组 hATX 的酶活性，其 IC50 为 14.2 nM[1]。
Autotaxin-IN-8 (24 h) 对人正常肺上皮 L132 细胞的细胞毒性较低，其 IC50 为 94.31 μM[1]。
Autotaxin-IN-8 (1 μM; 12 h) 可在 12 h 内显著抑制 A549 细胞的基础迁移、TGF-β 刺激的迁移以及 LPC 刺激的迁移[1]。
Autotaxin-IN-8 (1 μM; 48 h) 可在 48 h 内显著降低 MLg 细胞的自发性、TGF-β 诱导性及 LPC 诱导性胶原凝胶收缩[1]。

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

Autotaxin-IN-8 相关抗体:

Western Blot Analysis[1]

Cell Line: Human normal lung epithelial L132 cells
Concentration: 0.1-5.0 μM (concentration-dependent study); 0.5 μM (time-dependent study); 0.5 μM (LPC/LPA co-treatment pre-incubation); 0.5 μM (TGF-β co-treatment pre-incubation)
Incubation Time: 75 min (concentration-dependent study); 30-75 min (time-dependent study); 75 min pre-incubation + 15 min LPC/LPA stimulation (co-treatment); 3 h pre-incubation + 3 h TGF-β stimulation (co-treatment)
Result: Inhibited phosphorylation of p-JNK with an EC50 of 0.958 μM, p-p38 with an EC50 of 0.785 μM, and p-ERK1/2 with an EC50 of 0.297 μM, with marked inhibition at concentrations as low as 0.5 μM.
Inhibited phosphorylation of p-JNK with an estimated time of 35.4 min, p-p38 with an estimated time of 39.13 min, and p-ERK1/2 with an estimated time of 30.46 min, with effects observed within 30 min.
Suppressed LPC-induced activation of p-JNK, p-p38, and p-ERK1/2 but had no effect on LPA-induced activation.
Significantly reduced TGF-β-induced phosphorylation of JNK, ERK, and p38.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax T1/2 AUC0-last
Rat[1] 1 mg/kg p.o. 2.67 h 135.26 ng/mL 5.49 h 631.01
体内研究
(In Vivo)

Autotaxin-IN-8 (1 mg/kg；口服；单次) 可对雌性 Wistar 大鼠血浆中的 LPA18:2 实现高达 97% 的抑制率，且其抑制率维持在 75% 以上的时长可达 12 小时[1]。
Autotaxin-IN-8 (1-3 mg/kg；口服；每日一次；21 天) 可在 Bleomycin (HY-17565A) 诱导的肺纤维化小鼠模型中减少胶原沉积、纤维化标志物表达及炎症反应[1]。

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

Animal Model: C57BL/6 (male, 8 weeks old, bleomycin-induced pulmonary fibrosis)[1]
Dosage: 1 mg/kg; 3 mg/kg
Administration: p.o.; daily; 21 days
Result: Markedly reduced bleomycin-induced collagen deposition in lung tissue.
Decreased lung tissue expression of α-SMA and TGF-β.
Suppressed the bleomycin-induced increase in LPAR1 and p-ERK1/2.
Mitigated bleomycin-provoked inflammatory responses by reducing IL-1β and IL-6 expression in lung tissue.
分子量

449.90

Formula

C21H20ClN9O
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

Autotaxin-IN-8 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:

Autotaxin-IN-83058084-21-9Phosphodiesterase (PDE)p38 MAPKLPL ReceptorERKJNKLysophospholipid ReceptorExtracellular signal regulated kinasesc-Jun N-terminal kinaseA549 cellsp38bleomycin-induced pulmonary fibrosis mouse modelshuman plasmaLPA18:2pulmonary fibrosisERK1/2human normal lung epithelial L132 cellsautotaxinInhibitorinhibitorinhibit

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