2. Neuronal Signaling Metabolic Enzyme/Protease Apoptosis
  3. Imidazoline Receptor Mitochondrial Metabolism Caspase Lactate Dehydrogenase
  4. AGN 192403

AGN 192403 (BRD4780) 是一种强效且选择性的咪唑啉-1 (imidazoline-1) 受体拮抗剂，Ki 值为 42 nM。AGN 192403 也是一种 TMED9 抑制剂。AGN 192403 对星形胶质细胞的氧化毒性和线粒体抑制剂诱导的细胞毒性具有保护作用。AGN 192403 可抑制分化型胶质瘤细胞的增殖和迁移。AGN 192403 可用于胶质瘤和神经系统疾病的研究。

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AGN 192403

AGN 192403 Chemical Structure

CAS No. : 175521-95-6

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AGN 192403 的其他形式现货产品:

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AGN 192403 相关抗体

Top Publications Citing Use of Products

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AGN 192403 (BRD4780) is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 is also a TMED9 inhibitor. AGN 192403 shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 can be used for glioma tumor and neurological diseases research[1][2].

IC50 & Target[1]

Caspase-9

 

imidazoline-1 receptor

42 nM (Ki)

体外研究
(In Vitro)

AGN 192403 (0-25 μM，24 小时) 抑制 Naphthazarin (HY-N7526) 诱导的星形胶质细胞溶酶体不稳定及其导致的线粒体 (mitochondrial) 膜电位下降[1]。
AGN 192403 (10-100 μM，24 小时) 抑制抗霉素 A 和 Rotenone (HY-B1756) 诱导的星形胶质细胞线粒体膜电位下降、细胞色素 c 释放、caspase-9 活化以及最终的 LDH 释放[1]。
AGN 192403 (4-25 μM，14 天) 对胶质瘤干细胞 (GSC) 的自我更新具有显著的抑制作用，在最高浓度下几乎完全抑制了自我更新[2]。
AGN 192403 (0-25 μM，18-48 小时) 靶向 TMED9，降低 GSC 干性，减少 GSC 的迁移，并抑制 GSC 的致瘤功能[2]。
AGN 192403 (4-25 μM，0-8 天) 以剂量依赖的方式诱导患者来源的 GSC 细胞死亡[2]。
AGN 192403 (4-25 μM，48 小时-8 天) 抑制 TMED9，并在弥漫性内生性脑桥胶质瘤 (DIPG) 细胞中发挥抗肿瘤作用[2]。

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

AGN 192403 相关抗体:

Western Blot Analysis[2]

Cell Line: patient-derived GSCs
Concentration: 0, 4, 10, 25 μM
Incubation Time: 48 h
Result: Decreased TMED9 expression in a dose-dependent manner in three different patient-derived GSCs.

RT-PCR[2]

Cell Line: GSCs
Concentration: 10, 25 μM
Incubation Time: 48 h
Result: Showed a marked and dose dependent reduction in SOX2 expression.
Markedly reduced YKL40 expression.

Cell Migration Assay [2]

Cell Line: GSCs
Concentration: 10, 25 μM
Incubation Time: 18-20 h
Result: Dose-dependently reduced GSC migration.

Cell Viability Assay[2]

Cell Line: GSCs
Concentration: 4, 10, 25 μM
Incubation Time: 0, 1, 2, 3, 4, 5, 6, 7, 8 days
Result: Resulted in a dose-dependent induction of cell death, at multiple points over the course of one week.
体内研究
(In Vivo)

AGN 192403 (3000 μg/kg，静脉注射，单剂量预处理) 可以阻断咪唑啉-1受体，而不会改变大鼠的心率和血压的基线值[3]。

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

153.26

Formula

C10H19N
CAS 号
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

AGN 192403 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:

AGN 192403175521-95-6BRD4780AGN192403AGN-192403BRD 4780BRD-4780Imidazoline ReceptorMitochondrial MetabolismCaspaseLactate DehydrogenaseLDHImidazolineimidazoline-1 receptorsneuroprotectiveNaphthazarinAntimycin Aprimary astrocytesInhibitorinhibitorinhibit

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