2. TGF-beta/Smad MAPK/ERK Pathway
  3. TGF-β Receptor p38 MAPK
  4. J-1149

J-1149 是一种有效的 ALK5 抑制剂，IC50 值为 0.017 μM。J-1149 还表现出较弱的 p38α MAP 激酶抑制活性，IC50 值为 0.435 μM。J-1149可用于肝纤维化研究。

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J-1149 Chemical Structure

J-1149 Chemical Structure

CAS No. : 2883580-95-6

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J-1149 相关抗体

Top Publications Citing Use of Products

查看 TGF-β Receptor 亚型特异性产品:

查看所有亚型
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
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

J-1149 is a potent ALK5 inhibitor, with an IC50 value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC50 value of 0.435 μM. J-1149 can be used for liver fibrosis research[1].

IC50 & Target

ALK5

0.017 μM (IC50)

p38α MAPK

 

体外研究
(In Vitro)

J-1149 (compound 15g) (5-40 μM, 24 h) 可有效抑制 TGF-β 诱导的肝星状细胞 (HSC) 中的细胞外基质 (ECM) 沉积，并最终抑制 HSC 激活[1]。
J-1149 (20 μM, 24 h) 抑制 TGF-β 刺激的 α-SMA 和胶原蛋白 I 的表达[1]。

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

J-1149 相关抗体:

Western Blot Analysis[1]

Cell Line: LX-2 cells
Concentration: 20 μM
Incubation Time: 1 h prior to TGF-β stimulation for continuous 24 h
Result: Inhibited the expression of α-SMA and collagen I stimulated by TGF-β.
体内研究
(In Vivo)

J-1149 (compound 15g) (15 mg/kg, 口服给药, once) 表现出良好的药代动力学 (PK) 特征和良好的半衰期 (t1/2 = 9.14 h) [1]。

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

Animal Model: Sprague Dawley (SD) rats[1]
Dosage: 4 mg/kg (IV), 15 mg/kg (PO)
Administration: IV or PO, once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of J-1149 in male Sprague-Dawley rats[1].
IV (4 mg/kg) PO (15 mg/kg)
Tmax (h) 0.00 ± 0.00 0.11 ± 0.13
Cmax (ng/mL) 43,144 ± 35,001 1386 ± 882
AUC0-t (ng/mL∗h) 12,529 ± 978 1217 ± 20
AUC0-∞ (ng/mL∗h) 12,802 ± 1160 2667 ± 1136
t1/2 (h) 2.24 ± 1.05 9.14 ± 5.13
CL (mL/h/kg) 314 ± 28 6564 ± 3372
F (%) 2.59%
分子量

452.51

Formula

C25H24N8O
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

J-1149 相关分类

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  • 稀释计算器

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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:

J-11492883580-95-6J1149J 1149TGF-β Receptorp38 MAPKTransforming growth factor beta receptorsTGF-βα-SMAcollagen ILX-2 cellsliver fibrosishepatic stellate cellsInhibitorinhibitorinhibit

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