1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. HIF-1 inhibitor-5

HIF-1 inhibitor-5 (Compound 16e) 是一种有效的 HIF-1 抑制剂,其 IC50 为 2.38 μM。HIF-1 inhibitor-5 具有抗血管生成潜能。

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HIF-1 inhibitor-5 Chemical Structure

HIF-1 inhibitor-5 Chemical Structure

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查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HIF-1 inhibitor-5 (Compound 16e) is a potent HIF-1 inhibitor with an IC50 of 2.38 μM. HIF-1 inhibitor-5 possesses anti-angiogenic potential[1].

IC50 & Target

IC50: 2.38 μM (HIF-1)[1]

体外研究
(In Vitro)

HIF-1 inhibitor-5 (Compound 16e; 0-4 μM; 24 h) 抑制 A549 细胞迁移和侵袭[1]
HIF-1 inhibitor-5 (0-8 μM; 12 h) 阻断 VEGF 诱导的血管形成[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: A549 and HUVEC cells
Concentration: 0-128 μM
Incubation Time: 48 h
Result: Showed cytotoxic effects with IC50s of 8.883 μM and 19.599 μM for A549 and HUVEC cells, respectively.

Cell Migration Assay [1]

Cell Line: A549 cell
Concentration: 0, 2 and 4 μM
Incubation Time: 24 h
Result: The number of migrated A549 cells decreased significantly.

Cell Invasion Assay[1]

Cell Line: A549 cell
Concentration: 0, 2 and 4 μM
Incubation Time: 24 h
Result: Inhibited cell invasion at a concentration-dependent manner.
体内研究
(In Vivo)

HIF-1 inhibitor-5 (Compound 16e; 1.25-20 μM; s.c.; once) 抑制 VEGF 诱导的小鼠血管生成[1]

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

Animal Model: C57/bl6 female mice, VEGF-induced angiogenesis model[1]
Dosage: 1.25, 5 and 20 μM
Administration: 0.5 mL of matrix glue subcutaneously injected near the midline of abdomen
Result: Decreased the number of blood vessels.
Animal Model: SD rats
Dosage: 20 mg/kg
Administration: Intravenous administration (Pharmacokinetic Study)
Result: Pharmacokinetic parameters of HIF-1 inhibitor-5 (Compound 16e) in rats after intravenous administrationa[1]
Parameter iv (20 mg/kg) (n = 2)
Tmax (h) 0.033
Cmax (μmol/L) 7.06
T1/2 (h) 1.64
CL (mL/h) 2368.50
VZ (L) 5.59
AUC0-t (μmol•h/L) 5.27
AUC0-∞ (μmol•h/L) 8.88

aAfter administration, blood samples were collected at different time (0, 0.083, 0.17, 0.5, 1, 2, 4, 6 h). The combination of compounds in a ratio of 8% ethanol absolute, 4% Tween-80 and 88% normal saline was chosen for the intravenous injection formulation.
分子量

465.58

Formula

C28H35NO5

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

HIF-1 inhibitor-5 相关分类

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  • 稀释计算器

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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)
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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:
HIF-1 inhibitor-5
目录号:
HY-149260
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