2. Stem Cell/Wnt TGF-beta/Smad
  3. TGF-beta/Smad
  4. TGF-β1/Smad3-IN-1

TGF-β1/Smad3-IN-1 (Compound 5aa) 是 TGF-β1/Smad3 信号通路的抑制剂 (IC50=1.07 μM)。具有抗纤维活性和口服有效性。

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TGF-β1/Smad3-IN-1 Chemical Structure

TGF-β1/Smad3-IN-1 Chemical Structure

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TGF-β1/Smad3-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency[1].

体外研究
(In Vitro)

TGF-β1/Smad3-IN-1 (100-500 nM; 48 h) 导致 H2228 细胞的 TGF-β1 水平降低,比相同浓度的 Nintedanib (HY-50904) 现出更好的抑制作用[1]。
TGF-β1/Smad3-IN-1 (2-6 μM; 24 h) 表现出剂量依赖性抑制 p-Smad3 和 α-SMA 表达,显著抑制 NIH3T3 细胞迁移[1]。
TGF-β1/Smad3-IN-1 (3-10 μM; 72 h) 增加 NIH3T3 细胞中的 Cleave-casepase3 的表达,剂量依赖性的诱导细胞凋亡[1]。
TGF-β1/Smad3-IN-1 对于 NIH3T3 细胞的 IC50 为 1.07 μM。对于 TGFβ1 激活的 HFL1 细胞的 IC50 为 2.86 ± 0.014 μM。有效地抑制了活化标志物 α-SMA 的表达[1]。

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

TGF-β1/Smad3-IN-1 相关抗体:

Apoptosis Analysis[1]

Cell Line: NIH3T3
Concentration: 3, 7.5, 10 μM
Incubation Time: 72 h
Result: At the highest concentration of 10 μM, the total apoptosis rate of cells reached 91.79%, indicating that 5aa has a strong ability to induce apoptosis.
体内研究
(In Vivo)

TGF-β1/Smad3-IN-1 在 SD 大鼠中的生物利用度高于 Nintedanib (HY-50904)[1]。
TGF-β1/Smad3-IN-1 (p.o.; 100 mg/kg/; 第二到二十天) 处理博来霉素诱导的小鼠肺纤维化模型，可以抑制博莱霉素诱导的肺 TGFβ1和 HYP 的表达，减少细胞外间质沉积，减轻肺纤维化[1]。


药代动力学分析[1]

Route Dose (mg/kg) Tmax (h) t1/2 (h) Vz_F_obs (L/kg) MRT0~t (h) AUC0~t-Dobs (h·ng/mL/mg) F (%)
p.o. 10 3.01 ± 1.24 3.85 ± 0.31 / 5.117 ± 1.23 203.540 ± 4.7 15.96 ± 4.67
i.v. 1 0.029 ± 0.001 2.577 ± 0.33 19.636 ± 1.48 / 127.471 ± 25.41 /


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

Animal Model: Bleomycin-induced model of pulmonary fibrosis in mice[1]
Dosage: 100 mg/kg/
Administration: p.o.; day 2-20
Result: Significantly reduced α-SMA, fibronection and p-smad3 protein expression levels.
Significantly reduced TGFβ1 levels, more effective than Nintedanib.
Reduced hydroxyproline (HYP) levels.
分子量

578.68

Formula

C30H34N4O6S
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

TGF-β1/Smad3-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

TGF-β1/Smad3-IN-1TGF-beta/SmadTransforming growth factor betaAnti fibroticOral activitySD ratsInhibitorinhibitorinhibit

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