2. GPCR/G Protein
  3. Apelin Receptor (APJ)
  4. APJ antagonist-1

APJ antagonist-1 是一种 apelin 受体 (APJ) 拮抗剂。APJ antagonist-1 具有强效的 β-arrestin 抑制作用，IC50 为 3.1 μM。APJ antagonist-1 选择性抑制 APJ 过表达的癌细胞，并抑制 apelin 诱导的内皮细胞迁移。APJ antagonist-1 具有较高的代谢稳定性。APJ antagonist-1 可用于卵巢癌和肿瘤血管生成的研究。

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APJ antagonist-1

APJ antagonist-1 Chemical Structure

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APJ antagonist-1 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

APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC50 of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis[1].

体外研究
(In Vitro)

APJ antagonist-1 (Compound 21) (1 h) 的代谢稳定性显著高于 ML221 (HY-103254) (1 h 后血浆中残留 100%；肝微粒体 t1/2 = 5 min)[1]。
APJ antagonist-1 (12.5-100 μM, 3 days) 显著降低 OVCAR8 细胞和 HT-29 细胞活力[1]。
APJ antagonist-1 (30 μM, 8 h) 显著抑制了 apelin 诱导的 OVCAR3 细胞和 HUVEC 迁移[1]。

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

APJ antagonist-1 相关抗体:

Cell Migration Assay [1]

Cell Line: OVCAR3 cells and HUVECs
Concentration: 30 μM
Incubation Time: 8 h
Result: Significantly inhibited apelin-induced migration and the effect was comparable to or even better than ML211.
分子量

433.46

Formula

C18H15N3O6S2
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

APJ antagonist-1 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:

APJ antagonist-1APJ antagonist1APJ antagonist 1Apelin Receptor (APJ)APJ antagonistApelin receptor (APJ)ML221 analogsPlasma and liver microsomal stabilityStructure-activity relationship (SAR)Sulfonate linkageβ-arrestin inhibitionInhibitorinhibitorinhibit

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APJ antagonist-1
目录号：
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