2. Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. COX VEGFR
  4. (±)-Aiphanol

(±)-Aiphanol  (Synonyms: Aiphanol)

目录号: HY-152120
产品使用指南

摩尔计算器

(±)-Aiphanol 是一种新发现的 stilbenolignan 类化合物。(±)-Aiphanol 具有显著的抗炎活性，通过抑制 COX-1 和 COX-2 发挥作用。其对 COX-1 的抑制作用尤其强 (IC50 = 1.9 μM)，而对 COX-2 的作用相对较弱 (IC50= 9.9 μM)。(±)-Aiphanol 有效抑制 VEGFR2 (IC50=0.92 µM)。(±)-Aiphanol 通过抑制 VEGFR2 和 COX2 的活性来阻断血管生成，促进细胞凋亡。(±)-Aiphanol 是口服有效的。

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(±)-Aiphanol Chemical Structure

(±)-Aiphanol Chemical Structure

CAS No. : 578020-29-8

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(±)-Aiphanol 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

查看所有亚型
COX COX-1 COX-2 COX-3

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak[1].(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 µM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active[2].

IC50 & Target[1][2]

COX-1

1.9 μM (IC50)

COX-2

9.9 μM (IC50)

VEGFR2

0.92 μM (IC50)

体外研究
(In Vitro)

(±)-Aiphanol (7.5-30 μM; 6 h) 剂量依赖性的抑制 HUVECs 细胞的 VEGF 诱导的新血管形成。显著降低 HUVECs 细胞的 PGE2 和 VEGF 水平，这一效果在 COX2 沉默后消失。在抑制 HUVECs 细胞的 VEGF 诱导的管状结构形成方面比 Celecoxib (HY-14398) 效果更强[2]。
(±)-Aiphanol (7.5-30 μM; 6h) 显著抑制 CAM 的微血管生长，效果与 Bevacizumab (HY-P9906) 相当[2]。
(±)-Aiphanol 抑制 VEGFR3/FLT4，VEGFR2/KDR 和 VEGFR1/FLT1 的活性，同时对 PI3K-AKT 和 MAPK 通路中的某些激酶有中等或弱的抑制作用[2]。
(±)-Aiphanol (30 μM; 24 h) HUVECs 的增殖受到抑制，并诱导了细胞凋亡[2]。

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

(±)-Aiphanol 相关抗体:

Apoptosis Analysis[2]

Cell Line: HUVECs
Concentration: 30 μM
Incubation Time: 24 h
Result: Did not cause significant changes in cell cycle distribution but significantly increased apoptosis. Elevated the expression of P53 and BAX proteins.
体内研究
(In Vivo)

(±)-Aiphanol (30 mg/kg; p.o.; 单剂量) 显著抑制 MC38 同系小鼠模型中的肿瘤生长，肿瘤重量显著减少[2]。

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

Animal Model: MC38 syngeneic mouse model[2]
Dosage: 30 mg/kg
Administration: p.o.; single dose
Result: Increased apoptosis in tumor tissues and reduced the phosphorylation levels of VEGFR2, AKT, and ERK.
Significantly decreased the levels of vascular markers CD31 and factor VIII.
Lowered the levels of PGE2 in plasma and VEGF in tumor tissues.
Did not cause changes in body weight or the morphology of major organs.
分子量

452.45

Formula

C25H24O8
CAS 号
结构分类
初始来源
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

(±)-Aiphanol 相关分类

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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.

Keywords:

(±)-Aiphanol578020-29-8AiphanolCOXVEGFRCyclooxygenaseVascular endothelial growth factor receptorCOX inhibitorStilbenolignanAnti-inflammatoryAnti-angiogenesisTumor Growth InhibitorcancerInhibitorinhibitorinhibit

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