2. Neuronal Signaling
  3. Transthyretin (TTR)
  4. Transthyretin-IN-3

Transthyretin-IN-3 (compound 6) 是一种经过设计的苯并呋喃类似物。Transthyretin-IN-3 选择性地与血浆中转甲状腺素结合来抑制淀粉样蛋白聚集 (IC50=5.0±0.2 μM)。Transthyretin-IN-3 通过在其结构中的特定位置带有氯取代基，能够特异性且强力地结合到 TTR 的甲状腺素结合位点，这种结合能够阻止 TTR 四聚体解离为不稳定单体。

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Transthyretin-IN-3 Chemical Structure

Transthyretin-IN-3 Chemical Structure

CAS No. : 3008535-20-1

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Transthyretin-IN-3 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

Transthyretin-IN-3 (compound 6) is a designed benzofuran analogue. Transthyretin-IN-3 selectively binds to plasma transthyretin (TTR) to inhibit Amyloid aggregation (IC50=5.0±0.2 μM). Transthyretin-IN-3 can bind to TTR's thyroxine binding site specifically by carrying chlorine substituents at specific locations in its structure. This binding can prevent TTR tetramers from dissociating into unstable monomers[1].

体内研究
(In Vivo)

Transthyretin-IN-3 ( 0.1 mg/kg，iv；0.1 mg/kg，po；8 h) 对 SD 大鼠口服生物利用度 (BA) 为 66.8 %，与目前的有效治疗药物效果相当[1]。
Pharmacokinetic Analysis in SD rats[1]

Route Dose (mg/kg) C0/max (ng/mL) CLtot (mL/h/kg) Vdss (mL/kg) AUC0_8 (ng•h/mL) BA (%)
i.v. 0.1 1718 20.6 112 3726 /
p.o. 0.1 395 / / 2524 67.7

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

552.53

Formula

C17H11ClI2O3
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

Transthyretin-IN-3 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Transthyretin-IN-33008535-20-1Transthyretin (TTR)thyroxine-binding prealbuminTransthyretin amyloidosisDawley ratsSD ratsInhibitorinhibitorinhibit

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