OY-101

• 常用名: OY-101
• 英文名: OY-101
• CAS号: 41183-02-2
• 分子量: 433.54
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₇H₃₁NO₄
• 熔点: N/A
• 闪点: N/A

OY-101用途

OY-101是一种口服活性、强效和特异性P-糖蛋白(P-gp)抑制剂。OY-101能使耐药肿瘤增敏,有效逆转肿瘤多药耐药性。与汉防己碱(HY-13764)相比,OY-101在水溶性、细胞毒性和逆转活性方面有所改善[1]。

OY-101名称

• 英文名: (±)-O-benzyllaudanidine

OY-101生物活性

• 描述: OY-101是一种口服活性、强效和特异性P-糖蛋白(P-gp)抑制剂。OY-101能使耐药肿瘤增敏,有效逆转肿瘤多药耐药性。与汉防己碱(HY-13764)相比,OY-101在水溶性、细胞毒性和逆转活性方面有所改善[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 跨膜转运 >> P-糖蛋白
• 体外研究: OY-101型与长春新碱(HY-N0488A)对耐药细胞 Eca109/录像机表现出优异的协同抗癌作用,IC50为 9.9±1.3 nM＜sup＞[1]OY-101(0-5μM)对 Eca109/录像机细胞没有显著毒性,并且在 Eca109/录像机细胞中表现出显着增加的长春新碱(HY-N0488A)敏感性[1] 细胞活力测定[1]细胞系：Eca109/VCR细胞浓度：1.0、2.5和5.0μM孵育时间：48小时结果：抑制了Eca109-VCR细胞中长春新碱的增敏作用,分别达到约3.7、103.4和690.6倍的逆转活性。
• 体内研究: OY-101(30毫克/千克/2天,灌胃,持续 3.周)增加体内对长春新碱 (HY-N0488A)的致敏性,且无明显毒性[1] OY-101型(静脉给药 (3毫克/千克)和口服给药 (30毫克/千克)一次) 表现出良好的药代动力学[1] 动物模型：雌性裸鼠(4-5周龄,异种移植物模型,携带高表达Eca109/VCR细胞的P-gp)[1]剂量：30 mg/kg给药：IG,每2天1次,持续3周,尾静脉注射长春新碱(HY-N0488A)前1小时。治疗3周后,OY-101/长春新碱组合的肿瘤生长抑制率为79.13%,显著低于单一治疗组和载体组。动物模型：SD大鼠(8周龄,雄性,300-400 g)[1]剂量：3 mg/kg(IV),30 mg/kg(PO)给药：静脉和口服给药,一次(药代动力学分析)结果：OY-101在雄性Sprague-Dawley大鼠体内的药代动力学参数[1]。静脉注射(3 mg/kg)PO(30 mg/kg)Tmax(h)0.17±0.12 0.38±0.18 Cmax(ng/mL)1573.20±143.97 636.55±355.60 AUC0-t(ng/mL*h)2688.45±180.10 2665.45±450.92 t1/2(h)8.43±7.83 7.37±4.92 CL/F(L/kg/h)1.10±0.08 11.16±2.10 Vz/F(L/kg)12.84±11.33 111.27±56.82 F(%)7.65±2.15
• 参考文献:

  [1]. Zeng R, et al. Simplified Derivatives of Tetrandrine as Potent and Specific P-gp Inhibitors to Reverse Multidrug Resistance in Cancer Chemotherapy. J Med Chem. 2023 Mar 23;66(6):4086-4105.

OY-101物理化学性质

• 分子式: C₂₇H₃₁NO₄
• 分子量: 433.54
• 精确质量: 433.22500
• PSA: 40.16000
• LogP: 5.00100

OY-101靶点实验

查看更多实验

实验名称：Induction of apoptosis in vincristine resistant human Eca-109 cells assessed as necro... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251748

实验名称：Induction of apoptosis in vincristine resistant human Eca-109 cells assessed as necro... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251747

实验名称：Synergistic anticancer activity in vincristine resistant human Eca-109 cells assessed... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251750

实验名称：Inhibition of clone formation in vincristine resistant human Eca-109 cells at 2 uM in... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5251749

实验名称：Induction of apoptosis in vincristine resistant human Eca-109 cells assessed as late ... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251744

实验名称：Induction of apoptosis in vincristine resistant human Eca-109 cells assessed as late ... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251743

实验名称：Induction of apoptosis in vincristine resistant human Eca-109 cells assessed as necro... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251746

实验名称：Induction of apoptosis in vincristine resistant human Eca-109 cells assessed as late ... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251745

实验名称：Induction of apoptosis in vincristine resistant human Eca-109 cells assessed as early... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251740

实验名称：Induction of apoptosis in vincristine resistant human Eca-109 cells assessed as viabl... 来源：ChEMBL 靶标：ECa-109 cell line External Id：CHEMBL5251739

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OY-101英文别名

• 1-[3-Benzyloxy-4-methoxy-benzyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-isochinolin
• (+/-)-O-benzyl-laudanine
• (+/-)-O-benzyllaudanidine
• 1-(3-Benzyloxy-4-methoxy-benzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydro-isochinolin
• 1-(3-benzyloxy-4-methoxy-benzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydro-isoquinoline
• (+/-)-O-Benzyl-laudanin