WAY-388264-A

• 常用名: WAY-388264-A
• 英文名: WAY-388264-A
• CAS号: 393129-91-4
• 分子量: 296.17
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₁H₁₄BrN₅
• 熔点: N/A
• 闪点: N/A

WAY-388264-A用途

5-HT2B拮抗剂-1是一种口服活性5-HT2B受体拮抗剂,IC50值为33.4 nM。5-HT2B拮抗剂-1可用于研究以5-HT2B受体信号为特征的疾病,如肝细胞癌、心血管疾病或胃肠道疾病[1][2]。

WAY-388264-A名称

• 英文名: 5-HT2B antagonist-1

WAY-388264-A生物活性

• 描述: 5-HT2B拮抗剂-1是一种口服活性5-HT2B受体拮抗剂,IC50值为33.4 nM。5-HT2B拮抗剂-1可用于研究以5-HT2B受体信号为特征的疾病,如肝细胞癌、心血管疾病或胃肠道疾病[1][2]。
• 相关类别:
  研究领域 >> 癌症
  研究领域 >> 心血管疾病
  研究领域 >> 内分泌
  研究领域 >> 代谢疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
• 靶点实验:

  5-HT2B Receptor:33.4 nM (IC50)

• 体外研究: 5-HT2B拮抗剂-1(化合物5g)具有一些钠通道结合活性,IC50值在12.6至57.5μM范围内[1]。5-HT2B拮抗剂-1(复合物1-e)在CHO-K1细胞系中1μM处抑制5-HT2B受体活性低于50%[3]。
• 体内研究: 5-HT2B拮抗剂-1(化合物15)(口服灌胃,30 mg/kg)可显著降低肠易激综合征(IBS)大鼠的内脏超敏反应[2]。
• 参考文献:

  [1]. Xiang Ma, et al. Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5644

  [2]. Yu Zhou, et al. Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome. J Med Chem. 2016 Jan 28;59(2):707-20.

  [3]. Huang Niu, et al. 5-HT2B Antagonists. WO2015158214

WAY-388264-A物理化学性质

• 分子式: C₁₁H₁₄BrN₅
• 分子量: 296.17
• InChIKey: VDTGYRUIQQDQTL-UHFFFAOYSA-N
• SMILES: Cc1sc2ncnc(N3CCN(S(=O)(=O)c4ccc(C(C)(C)C)cc4)CC3)c2c1C
• 储存条件: 2-8°C

WAY-388264-A靶点实验

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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

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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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