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  3. SRI-35241

SRI-35241 是一种血小板反应蛋白 TSP-1 抑制剂,其针对人源靶点的 pIC50 为 8.12 nM。SRI-35241 可抑制 TSP-1 与潜伏转化生长因子-β 相关肽 (LAP) 的结合,阻断 TGF-β 的激活。SRI-35241 具有一定时效性,经静脉给药后的血浆半衰期为 1.8 h。SRI-35241 可用于多发性骨髓瘤和纤维化疾病的研究。

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SRI-35241

SRI-35241 Chemical Structure

CAS No. : 2307429-54-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SRI-35241 is a thrombospondin TSP-1 inhibitor with a pIC50 of 8.12 nM against human targets. SRI-35241 inhibits the binding of TSP-1 to latent transforming growth factor-β-associated peptide (LAP) and blocks the activation of TGF-β. SRI-35241 shows a certain time-dependent property, with a plasma half-life of 1.8 h after intravenous administration. SRI-35241 can be used for the research of multiple myeloma and fibrotic diseases[1].

体外研究
(In Vitro)

SRI-35241 可抑制人骨髓瘤细胞中 TSP-1 介导的 TGF-β 激活,其 pIC50 为 8.12 nM[1]
SRI-35241 (10 nM; 10 min) 在间接结合 ELISA 实验中,可抑制重组 LAP 与重组 TSP-1 的 1 重复序列 (P123) 的结合,抑制率约为 85%[1]
SRI-35241 在大鼠肝微粒体中的半衰期为 170 min,在人肝微粒体中的半衰期大于 300 min,表明其相较于母本化合物具有更优的微粒体稳定性[1]

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

体内研究
(In Vivo)

SRI-35241 相较于母本化合物展现出更优的体内血浆稳定性,其静脉注射给药的半衰期为 1.9 h,腹腔注射给药的半衰期为 7 h,进而使血浆浓度持续维持在其 pIC50 水平以上[1]

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

分子量

258.32

Formula

C11H22N4O3

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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  • 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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SRI-35241
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HY-182612
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