Bioactivity | P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells[1]. |
Target | IC50: 1.6 nM (P-glycoprotein), 600 nM (BCRP) |
Name | P-gp/BCRP-IN-2 |
Formula | C32H35N3O6 |
Molar Mass | 557.64 |
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]. Braconi L, et al. Tetrazole and oxadiazole derivatives as bioisosteres of tariquidar and elacridar: New potent P-gp modulators acting as MDR reversers. Eur J Med Chem. 2023 Nov 5;259:115716.. |