(R)-OY-101

(R)-OY-101 is an orally active and specific inhibitor of P-gp. (R)-OY-101 increases tumor sensitivity to anticancer agents. (R)-OY-101 has good activity in reversing tumor resistance and promoting apoptosis and can be used in cancer related research[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

(R)-OY-101 增加了长春新碱 (Vincristine；HY-N0488A) 对 Eca109/VCR 细胞的细胞毒性，IC50 值为 43.8 nM[1]。

OY-101 在 SD 大鼠中的药代动力学 (PK) 参数[1] 备注：(R)-OY-101 是 OY-101 的一种立体构型。 Administration manner Tmax (h) Cmax (ng/mL) λz (1/h) T1/2 (h) MRT0-inf (h) AUC0-t (ng /mL•h) AUC0-inf (ng /mL•h) AUMC0-inf (ng /mL•h2) Vz/F (L/kg) Cl/F (L/kg/h) F (%) Intravenous injection 0.17±0.12 1573.20±143.97 0.15±0.13 8.43±7.83 2.68±0.47 2688.45±180.10 2742.45±218.99 7391.35±1874.05 12.84±11.33 1.10±0.08 Oral gavage 0.38±0.18 636.55±355.60 0.12±0.08 7.37±4.92 4.89±1.01 2665.45±450.92 2737.40±515.20 131110.55±237.09 111.27±56.82 11.16±2.10 7.65±2.15

[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.