2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. PI3K-001

PI3K-001 是一种组织蛋白酶 B 响应型前药和抗纤维化剂。PI3K-001 可在纤维化肺病灶中经组织蛋白酶 B 介导的 Val-Ala 连接子切割，释放出具有活性的 PI3K 抑制剂有效载荷，而在健康组织中保持稳定。PI3K-001 可改善纤维化肺组织中的胶原沉积、组织塌陷和肺泡损伤。PI3K-001 可用于肺纤维化的研究。

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PI3K-001

PI3K-001 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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Customer Review

PI3K-001 相关抗体

Top Publications Citing Use of Products

查看 Cathepsin 亚型特异性产品:

查看所有亚型
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K-001 is a cathepsin B-responsive prodrug and antifibrotic agent. PI3K-001 undergoes cathepsin B-mediated cleavage of the Val-Ala linker in fibrotic lung lesions to release an active PI3K inhibitor payload, while it remains stable in healthy tissues. PI3K-001 improves collagen deposition, tissue collapse and alveolar injury in fibrotic lung tissues. PI3K-001 is applicable for the research of pulmonary fibrosis[1].

体外研究
(In Vitro)

PI3K-001 (50 μM; 30 min at 37 °C) 在人源和小鼠血浆中与白蛋白的结合率均超过 97%[1]。
PI3K-001 (50 μM; 1-7 days at 37 °C) 表现出高血浆稳定性，在 37 °C 条件下于人源和鼠源血浆中孵育 7 天的过程中，其活性载荷 P001 的释放量不足 1%[1]。

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

PI3K-001 相关抗体:
体内研究
(In Vivo)

PI3K-001 (9.5 mg/kg; i.v.; single dose) 可实现 P001 向纤维化肺组织的靶向递送，并使药物在肺组织中的留存时间至少达到 18 h[1]。
PI3K-001 (25 mg/kg; i.v.; once every 7 days; 2 total doses) 在博来霉素诱导的肺纤维化小鼠模型中展现出更优异的抗纤维化功效，相较于母药 P001，其可显著提升小鼠存活率、减轻体重下降程度并降低肺纤维化标志物水平[1]。
PI3K-001 (3 mg/kg; i.v.; single dose) 在健康 SD 大鼠中展现出更优的药代动力学特性，其 Cmax 较母药 P001 高 10 倍，AUC 高 7 倍，提示全身暴露量提升且循环时间延长[1]。

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

Animal Model: C57BL/6 (male, 20-22 g, bleomycin-induced pulmonary fibrosis)[1]
Dosage: 9.5 mg/kg
Administration: i.v.; single dose
Result: Delivered P001 to lung tissue at a concentration significantly higher than the parent P001 group at 6 h post-administration.
Maintained detectable P001 in lung tissue at up to ~50 ng/g at 18 h post-administration, while P001 was nearly undetectable in lung tissue.
Animal Model: C57BL/6 (male, bleomycin-induced pulmonary fibrosis)[1]
Dosage: 25 mg/kg
Administration: i.v.; once every 7 days; 2 total doses
Result: Significantly improved mouse survival compared to the P001 group.
Reduced body weight loss relative to the P001 group.
Produced statistically significant reductions in bleomycin-induced increases in lung weight and lung index, with greater improvement than P001 and the positive control nintedanib.
Significantly reduced lung collagen deposition and preserved alveolar structure, with lung tissue morphology closer to normal than the P001 group, as shown by Masson and H&E staining.
分子量

1704.95

Formula

C82H111F2N11O22S2
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

PI3K-001 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.

Keywords:

PI3K-001CathepsinEPR effectalbuminalveolar damagemouse plasmacollagen depositionpulmonary fibrosisbleomycin-induced pulmonary fibrosis mouse modelcathepsin Bhuman plasmafibrotic lung lesionsInhibitorinhibitorinhibit

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目录号：
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