2. GPCR/G Protein
  3. Apelin Receptor (APJ)
  4. YL-GB063

YL-GB063 是一种 Apelin 受体 (APJ) 拮抗剂。YL-GB063 可抑制 Apelin 诱导的 APJ β-arrestin 招募 (HTLA 细胞中 IC50 为 3.1 μM)。YL-GB063 对卵巢癌具有抗癌活性。

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YL-GB063

YL-GB063 Chemical Structure

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Customer Review

YL-GB063 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

YL-GB063 is an Apelin receptor (APJ) antagonist. YL-GB063 inhibits Apelin-induced APJ β-arrestin recruitment (IC50 of 3.1 μM in HTLA cells). YL-GB063 has anti-cancer activity against ovarian cancer[1].

体外研究
(In Vitro)

YL-GB063 (30 min) 可强效抑制瞬时转染 HTLA 细胞中 Apelin 诱导的 APJ β-arrestin 招募，其 IC50 为 3.1 μM[1]。
YL-GB063 在小鼠肝微粒体和人肝微粒体中的半衰期分别为 14.1 min 和 26.7 min[1]。
YL-GB063 (12.5-50 μM; 3 天) 可抑制 OVCAR8 卵巢癌细胞的活力[1]。
YL-GB063 (30 μM; 8 h) 完全抑制 Apelin 诱导的转染 APJ 的 HUVEC-APJ 内皮细胞迁移[1]。

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

YL-GB063 相关抗体:

Cell Viability Assay[1]

Cell Line: OVCAR8 ovarian cancer cells
Concentration: 12.5, 25, 50 μM
Incubation Time: 3 days (daily treatment)
Result: Inhibited OVCAR8 cell viability with an IC50 of 23.2 μM and achieved 96.0% maximal inhibition.
体内研究
(In Vivo)

YL-GB063 (100 mg/kg；腹腔注射；每日) 可在原位卵巢癌异种移植小鼠模型中显著将中位生存期延长至 43 天，减少腹水形成和疾病进展[1]。

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

Animal Model: athymic nude mice (female, 6−8 weeks old)[1]
Dosage: 100 mg/kg
Administration: i.p.; daily
Result: Prolonged median survival time to 43 days (control: 30 days).
Reduced abdominal circumferences significantly by day 21 compared to control and ML221 groups.
Decreased metastatic tumor nodule count compared to control group.
Reduced ascites incidence to 4 of 7 mice (control: all mice).
分子量

453.88

Formula

C17H12ClN3O6S2
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

YL-GB063 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:

YL-GB063Apelin Receptor (APJ)apelin receptorOVCAR8 ovarian cancer cellsOVCAR3 ovarian cancer cellsAPJOVCAR8-APJ ovarian cancer cellsOVCAR8-EV cellsβ-arrestinHTLA cellsorthotopic ovarian cancer xenograft mouse modelHUVEC-APJ endothelial cellsInhibitorinhibitorinhibit

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Inquiry Information

产品名称：
YL-GB063
目录号：
HY-181540
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