| Bioactivity | OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764)[1]. |
| Invitro | OY-101 与Vincristine (HY-N0488A) 对耐药细胞 Eca109/VCR 表现出优异的协同抗癌作用，IC50 为 9.9 ± 1.3 nM[1]。OY-101 (0-5 μM) 对 Eca109/VCR 细胞没有显著毒性，并且在 Eca109/VCR 细胞中表现出显着增加的Vincristine (HY-N0488A) 敏感性[1]。 Cell Viability Assay[1] Cell Line: |
| In Vivo | OY-101 (30 mg/kg/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 (静脉给药 (3 mg/kg) 和口服给药 (30 mg/kg)；一次) 表现出良好的药代动力学[1]。 Animal Model: |
| Name | OY-101 |
| CAS | 41183-02-2 |
| Formula | C27H31NO4 |
| Molar Mass | 433.54 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |