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Safironil

Safironil

产品编号 T67961   CAS 134377-69-8

safironil 是一种新型抗纤维化化合物,是胶原蛋白合成的竞争性抑制剂。safironil 在体外实验中对由胶原蛋白I mRNA 或平滑肌α-actin 水平监测的成纤维细胞的激活,以及由I 型和III 型胶原蛋白和层粘连蛋白生产判断的纤维生成有抑制作用。safironil 在不改变总羟脯氨酸的情况下对肝脏肉芽肿的大小没有影响,但通过增加III 型和减少I 型胶原的沉积改变了纤维化的模式。

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Safironil Chemical Structure
Safironil, CAS 134377-69-8
规格 价格/CNY 货期 数量
1 mg ¥ 680 现货
5 mg ¥ 1,600 现货
10 mg ¥ 2,390 现货
25 mg ¥ 3,960 现货
50 mg ¥ 5,760 现货
100 mg ¥ 7,860 现货
500 mg ¥ 15,800 现货
1 mL * 10 mM (in DMSO) ¥ 1,490 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Paclitaxel限时半价
产品目录号及名称: Safironil (T67961)
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纯度: 99.51%
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生物活性
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存储 & 溶解度
参考文献
产品描述 safironil is a novel antifibrotic compound and a competitive inhibitor of collagen synthesis. safironil inhibited in vitro experiments on fibroblast activation monitored by collagen I mRNA or smooth muscle alpha-actin levels, and fibrogenesis as judged by type I and type III collagen and laminin production. safironil had no effect on the size of liver granulomas without altering total hydroxyproline, but altered the pattern of fibrosis by increasing type III and decreasing type I collagen deposition.
体外活性 HOE 77, Safironil, and S 4682 are inhibitors of prolyl 4-hydroxylase, which is essential for thecollagen formation. Although HOE 77, Safironil, and S 4682 seem to work by inhibiting HSC activation, further studies will be required before their clinical application. alpha-Tocopherol, retinyl palmitate, and silybinin reduce lipid peroxidation and attenuate HSC activation in experimental models.[2]
体内活性 The present studies evaluate the mechanism of action of two novel antifibrotic compounds, HOE 077 and Safironil, which were designed as competitive inhibitors of collagen protein synthesis. Stellate cell activation, rather than collagen synthesis, proved to be the target of both HOE 077 and Safironil in the intact liver. In culture, the drugs not only prevented the activation of stellate cells but also accelerated their deactivation. They were no more effective in co-cultures containing hepatocytes than in pure stellate cell cultures, indicating that metabolic conversion of HOE 077 was not required. Interestingly, the response of cells from females was greater than that of male cells, leading to the conclusion that stellate activation is sexually dimorphic. This finding may be relevant to the observation that fibrosis in chronic viral hepatitis progresses less rapidly and that hepatocellular carcinoma is less frequent in females than in males.[1]
分子量 309.36
分子式 C15H23N3O4
CAS No. 134377-69-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 30 mg/mL (96.97 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2325 mL 16.1624 mL 32.3248 mL 80.812 mL
5 mM 0.6465 mL 3.2325 mL 6.465 mL 16.1624 mL
10 mM 0.3232 mL 1.6162 mL 3.2325 mL 8.0812 mL
20 mM 0.1616 mL 0.8081 mL 1.6162 mL 4.0406 mL
50 mM 0.0646 mL 0.3232 mL 0.6465 mL 1.6162 mL

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TargetMol Library Books参考文献

1. Wang YJ, et al. Two novel antifibrotics, HOE 077 and Safironil, modulate stellate cell activation in rat liver injury: differential effects in males and females. Am J Pathol. 1998;152(1):279-287. 2. Shimizu I. Antifibrogenic therapies in chronic HCV infection. Curr Drug Targets Infect Disord. 2001;1(2):227-240.

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 经典已知活性库 已知活性化合物库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Safironil 134377-69-8 Others Inhibitor inhibitor inhibit

 

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