BX430

• 常用名: BX430
• 英文名: BX 430
• CAS号: 688309-70-8
• 分子量: 413.107
• 密度: 1.7±0.1 g/cm3
• 沸点: 395.4±42.0 °C at 760 mmHg
• 分子式: C₁₅H₁₅Br₂N₃O
• 熔点: N/A
• 闪点: 192.9±27.9 °C

BX430用途

BX430 是一种有效且选择性的非竞争性的人 P2X4 受体通道变构拮抗剂,IC50 为 0.54 μM。 BX430 具有物种特异性。BX430 用于慢性疼痛和心血管疾病。

BX430名称

• 英文名: 1-(2,6-Dibromo-4-isopropylphenyl)-3-(3-pyridinyl)urea

BX430生物活性

• 描述: BX430 是一种有效且选择性的非竞争性的人 P2X4 受体通道变构拮抗剂,IC50 为 0.54 μM。 BX430 具有物种特异性。BX430 用于慢性疼痛和心血管疾病。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钙通道
  研究领域 >> 心血管疾病
  信号通路 >> 跨膜转运 >> P2X受体
• 靶点实验:

  IC50: 0.54 μM (human P2X4 receptor channels)[1]

• 体外研究: BX430实际上对所有其他P2X亚型,即P2X1-P2X3、P2X5和P2X7,在其IC50的10-100倍时没有功能影响[1]。BX430是斑马鱼P2X4的有效拮抗剂,但对大鼠和小鼠P2X4同源基因无影响[1]。用thapsigargin+BX430处理的P2X4表达细胞显示ATP引起的细胞内钙升高显著减少[1]。BX430(5μM)显著降低THP-1细胞ATP诱发的细胞内钙反应幅度[1]。
• 参考文献:

  [1]. Ase AR, et al. Identification and characterization of a selective allosteric antagonist of human P2X4 receptor channels. Mol Pharmacol. 2015 Apr;87(4):606-16.

  [2]. Sophocleous RA, et al. Pharmacological and genetic characterisation of the canine P2X4 receptor. Br J Pharmacol. 2020 Feb 4.

BX430物理化学性质

• 密度: 1.7±0.1 g/cm3
• 沸点: 395.4±42.0 °C at 760 mmHg
• 分子式: C₁₅H₁₅Br₂N₃O
• 分子量: 413.107
• 闪点: 192.9±27.9 °C
• 精确质量: 410.958160
• LogP: 4.56
• InChIKey: JFNKIJKRXKPQCC-UHFFFAOYSA-N
• SMILES: CC(C)c1cc(Br)c(NC(=O)Nc2cccnc2)c(Br)c1
• 外观性状: 白色至淡黄色固体
• 蒸汽压: 0.0±0.9 mmHg at 25°C
• 折射率: 1.679
• 储存条件: 2-8°C，密封，干燥

BX430安全信息

• 危害码 (欧洲): Xn

BX430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

实验名称：Antagonist activity at human P2X4R transfected in 1321N1 cells assessed as inhibition... 来源：ChEMBL 靶标：P2X purinoceptor 4 External Id：CHEMBL4415958

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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：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

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

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BX430英文别名

• 1-(2,6-Dibromo-4-isopropylphenyl)-3-(3-pyridinyl)urea
• N-(2,6-dibromo-4-isopropylphenyl)-N'-(3-pyridinyl)urea