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  3. Progranulin modulator-1

Progranulin modulator-1是一种口服有效的前颗粒蛋白 (progranulin, PGRN) 分泌增强剂。Progranulin modulator-1增强对BV-2效力来提高PGRN水平的且对hERG有抑制作用,细胞毒性低,对 PGRN 的 EC50 和 hERG 的 IC50 分别为 83, 3100 nM。

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Progranulin modulator-1 Chemical Structure

Progranulin modulator-1 Chemical Structure

CAS No. : 2641013-11-6

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on hERG and Low cytotoxicity, the PGRN EC50 and hERG IC50 were 83 and 3100 nM, respectively[1].

IC50 & Target

EC50: 83 nM (PGRN); IC50: 3100 nM (hERG)

体外研究
(In Vitro)

Progranulin modulator-1 (Compound 60) 的流出率 (ER) 值 <2,表明不是 MDR 的底物,并显示具有高脑组织结合力和最高的代谢稳定性[1]

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

体内研究
(In Vivo)

Progranulin modulator-1 (Compound 60) (i.v.: 1 mg/kg, p.o.: 10 mg/kg) 具有良好的小鼠 PK 图谱,具有较高的生物利用度和半衰期,口服利用度能达到 99%,显示 Kpuu>1,表明在用药后 8 小时内大脑中的富集度非常高,用相对较低的 Progranulin modulator-1 的剂量就能达到调节作用[1]

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

分子量

369.41

Formula

C21H21F2N3O

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

Progranulin modulator-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.

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产品名称:
Progranulin modulator-1
目录号:
HY-153690
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