1. TGF-beta/Smad
  2. TGF-β Receptor
  3. TJN-331

TJN-331 是一种强效且口服有效的 TGF-β1 抑制剂。TJN-331 通过抑制 TGF-β1 的产生,改善大鼠抗肾小球基底膜 (GBM) 肾炎,从而减少肾小球毛细血管外增生。TJN-331 可抑制 ddY 小鼠实验性 IgA 肾病模型中的系膜扩张。TJN-331 可用于肾炎和 IgA 肾病的研究[1][2]

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TJN-331

TJN-331 Chemical Structure

CAS No. : 219964-53-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TJN-331 is a potent and orally active TGF-β1 Inhibitor. TJN-331 ameliorates anti-glomerular basement membrane (GBM) nephritis in rats by inhibitng TGF-β1 production, thereby reducing extracapillary proliferation in glomeruli. TJN-331 inhibits mesangial expansion in experimental IgA nephropathy in ddY mice. TJN-331 can be used for the research of nephritis and IgA nephropathy[1][2].

体外研究
(In Vitro)

TJN-331 (1-50 μmol/L;24-48 小时) 剂量依赖性地抑制总 TGF-β1 和成熟 TGF-β1 的产生,逆转 Smad 2 和 Smad 3 mRNA 表达的降低,并抑制抗 GBM 肾炎大鼠分离肾小球中纤溶酶原 mRNA 的表达[1]
TJN-331 (10-100 μmol/L;48 小时) 剂量依赖性地抑制 ConA 刺激的脾细胞中 TGF-β1 的产生[2]

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

体内研究
(In Vivo)

TJN-331 (0.1、0.5 和 2.0 mg/kg;口服给药;从第 21 天至第 41 天每日一次;持续 21 天) 在抗 GBM 诱导的肾炎大鼠模型中,能够减少蛋白尿和组织病理学改变,并抑制 TGF-β1 蛋白的产生及其在肾小球中的阳性表达区域[1]
TJN-331 (0.1、0.5 和 2.0 mg/kg;口服给药;从第 10 周至第 15 周每日一次;持续 5 周) 可改善小鼠 IgA 肾病模型中肾功能并减轻肾小球的组织病理学改变[2]

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

Animal Model: Male SD rats injected with goat γ-globulin and goat anti-rat GBM serum[1]
Dosage: 0.1, 0.5, and 2.0 mg/kg
Administration: p.o.; daily for 21 days from day 21 to day 41
Result: Prevented urinary protein excretion at 2 mg/kg from day 30 to day 41, and showed significant inhibition only at day 35 at 0.5 mg/kg. showed a tendency to inhibit nephritis induced increase in serum creatinine levels. Inhibited crescent formation and adhesion in the anti-GBM nephritic glomeruli at 2 mg/kg. Inhibited the increase of a-Smooth Muscle Actin (SMA) and TGF-β1-positive areas. Inhibited the increase in glomerular production of mature at 2 mg/kg.
Animal Model: Male ddY mice (7-week-old) induced by oral administration of bovine γ-globulin, followed by reticuloendothelial blocking by colloidal carbon injection and heminephrectomy.[2]
Dosage: 0.1, 0.5, and 2.0 mg/kg
Administration: p.o.; daily for 5 weeks (from week 10 to week 15 after induction)
Result: Inhibited increases in the mesangial matrix index and the number of nuclei per glomerular cross-section. Prevented increase in glomerular TGF-β1 staining without affecting IgA deposition. Did not influence urine volume during the experiments.
分子量

326.39

Formula

C19H22N2O3

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
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  • 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.

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产品名称:
TJN-331
目录号:
HY-178850
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