(+)-槐定啶

• 常用名: (+)-槐定啶
• 英文名: sophoridine
• CAS号: 83148-91-8
• 分子量: 248.36
• 密度: 1.164 g/cm3
• 沸点: 396.738ºC at 760 mmHg
• 分子式: C₁₅H₂₄N₂O
• 熔点: N/A
• 闪点: 172.748ºC

(+)-槐定啶用途

d-Sophoridine((+)-Sphoridine)是Sophoridin(HY-N1373)的右旋异构体,后者是从豆科植物苦参中分离出的喹啉类生物碱。Sophoridine诱导细胞凋亡。Sophoridine有可能成为一种新的、有效的、选择性的胰腺癌候选抗肿瘤药物,具有良好的耐受性[1]。

(+)-槐定啶名称

• 中文名: 槐定碱
• 英文名: Sophoridine

(+)-槐定啶生物活性

• 描述: d-Sophoridine((+)-Sphoridine)是Sophoridin(HY-N1373)的右旋异构体,后者是从豆科植物苦参中分离出的喹啉类生物碱。Sophoridine诱导细胞凋亡。Sophoridine有可能成为一种新的、有效的、选择性的胰腺癌候选抗肿瘤药物,具有良好的耐受性[1]。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
• 体外研究: Sophoridine(0-500μM；48小时)对人胰腺癌、胃癌、肝癌、结肠癌、胆囊癌和前列腺癌细胞的生长具有显著的抑制作用,IC50值约为20μM至200μM[1]。Sophoridine(0-20μM；48小时)使Miapaca-2细胞中的S期细胞群从26.23%(对照)增加到38.67%,使PANC-1细胞中的细胞群从29.56%(对照)提高到39.16%,分别增加了约1.5倍和1.3倍[1]。Sophoridine(0-20μM；48小时)显著增加bad和bax水平,降低bcl-2和bcl-xl水平,bax/bcl-2比值显著增加[1]。
• 体内研究: Sophoridine(腹膜内注射；20或40 mg/kg；21天)可抑制异种移植物胰腺肿瘤的生长[1]。
• 参考文献:

  [1]. Xu Z, et al. Sophoridine induces apoptosis and S phase arrest via ROS-dependent JNK and ERK activation in human pancreatic cancer cells. J Exp Clin Cancer Res. 2017 Sep 11;36(1):124.

(+)-槐定啶物理化学性质

• 密度: 1.164 g/cm3
• 沸点: 396.738ºC at 760 mmHg
• 分子式: C₁₅H₂₄N₂O
• 分子量: 248.36
• 闪点: 172.748ºC
• 精确质量: 248.18900
• PSA: 23.55000
• LogP: 1.74750
• InChIKey: ZSBXGIUJOOQZMP-UHFFFAOYSA-N
• SMILES: O=C1CCCC2C3CCCN4CCCC(CN12)C34
• 外观性状: 白色针状结晶粉末
• 储存条件: 2-8°C，干燥、避光、密封

(+)-槐定啶靶点实验

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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：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

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：A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS979

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

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：Primary Screen Inhibitors of CD40 Signaling in BL2 Cells Measured in Cell-Based Syste... 来源：Broad Institute 靶标：N/A External Id：7124-01_Inhibitor_SinglePoint_HTS_Activity

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(+)-槐定啶英文别名

• matridin-15-one
• (2R,3R)-2,3-bis(4-hydroxy-3-methoxybenzyl)-4-butanolide
• S-GINSENOSIDE RG3
• (2R,3R)-2,3-bis(4-hydroxy-3-methoxybenzyl)butyrolactone
• (3R,4R)-rel-Dihydro-3,4-bis[(4-hydroxy-3-methoxyphenyl)methyl]-2(3H)-furanone
• (E)-3,4-di[(4-hydroxy-3-methoxyphenyl)methyl]dihydro-2(3H)-furanone
• SOPHORIDINE (REFERENCE GRADE)
• rac Matairesinol
• (8R,8'R)-(-)-matairesinol
• Allomatrine
• trans-Dihydro-3,4-bis[(4-hydroxy-3-methoxyphenyl)methyl]-2(3H)-furanone