84-B10

• 常用名: 84-B10
• 英文名: 84-B10
• CAS号: 698346-43-9
• 分子量: 473.44
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₅H₂₂F₃NO₅
• 熔点: N/A
• 闪点: N/A

84-B10用途

84-B10是3-苯基戊二酸衍生物。84-B10抑制顺铂(HY-17394)诱导的管状铁下垂。84-B10减轻顺铂诱导的线粒体损伤和氧化应激。84-B10改善顺铂诱导的急性肾损伤(AKI)[1]。

84-B10名称

• 英文名: 84-B10

84-B10生物活性

• 描述: 84-B10是3-苯基戊二酸衍生物。84-B10抑制顺铂(HY-17394)诱导的管状铁下垂。84-B10减轻顺铂诱导的线粒体损伤和氧化应激。84-B10改善顺铂诱导的急性肾损伤(AKI)[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞凋亡 >> Ferroptosis
• 体外研究: 84-B10(10-100μM；2小时)以剂量依赖性方式抑制顺铂诱导的肾小管上皮细胞铁死亡[1]。 84-B10(40μM；2小时; TKPT公司细胞) 恢复顺铂诱导的线粒体结构损伤和功能障碍[1]。 84-B10(40μM；2小时; TKPT公司细胞) 减轻顺铂诱导的 阿吉中 线粒体活性氧诱导的氧化应激[1]。 84-B10(40μM；2小时; TKPT公司细胞) 通过消除 线粒体活性氧和恢复线粒体稳态来减轻顺铂诱导的上皮细胞损伤[1]。 Western Blot分析[1]细胞系：管状上皮细胞浓度：10、20、30、40、50和100μM培养时间：2小时结果：NRF2、SLC7A11和GPX4水平以剂量依赖性方式增加。Western印迹分析[1]细胞系：TKPT细胞浓度：40μM孵育时间：2小时结果：以剂量依赖的方式增加OM孔蛋白、IMS Cyt c、IM CVa、IM Core 1和Matrix CypD的水平。
• 体内研究: 84-B10(5-15 mg/kg；腹腔注射)减轻顺铂诱导的小鼠急性肾损伤[1]。 动物模型：急性肾损伤的雄性C57BL/6小鼠[1]剂量：5、10和15 mg/kg给药：腹腔注射结果：顺铂暴露小鼠的sCr和BUN水平降低。以剂量依赖的方式减轻肾小管形态学异常。NGAL和KIM-1水平呈剂量依赖性降低。降低Lcn2(编码NGAL)和Havcr1的转录水平。
• 参考文献:

  [1]. Fan J, et, al. A novel 3-phenylglutaric acid derivative (84-B10) alleviates cisplatin-induced acute kidney injury by inhibiting mitochondrial oxidative stress-mediated ferroptosis. Free Radic Biol Med. 2023 Jan;194:84-98.

84-B10物理化学性质

• 分子式: C₂₅H₂₂F₃NO₅
• 分子量: 473.44
• InChIKey: UMUXAMJXLBOQNN-UHFFFAOYSA-N
• SMILES: COc1ccc(Oc2ccc(C(F)(F)F)cc2NC(=O)CC(CC(=O)O)c2ccccc2)cc1

84-B10靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

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实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

实验名称：Absorbance-based primary biochemical high throughput screening assay to identify acti... 来源：The Scripps Research Institute Molecular Screening Center 靶标：caspase-3 preproprotein [Homo sapiens] External Id：PROCASPASE3_ACT_EPIABS_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule modulators of NR3A 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：SBCCG-A1015-NR3A-Primary-Assay

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