P-glycoprotein Substrate

Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC₅₀ of 6.8 nM. Carmegliptin hydrochloride binds to the S1 pocket of DPP‑IV, blocks the degradation of GLP‑1, potentiates endogenous GLP‑1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus.

10S,13aR-Antofine N-oxide is a phenanthroindolizidine N-oxide alkaloid and cytotoxic agent found in Cynanchum vincetoxicum. 10S,13aR-Antofine N-oxide exerts cytotoxic effects in drug-sensitive (KB-3-1, IC₅₀ = 0.11 μM) and multi-drug-resistant (KB-V1, IC₅₀ = 0.16 μM) carcinoma cells. 10S, 13aR-Antofine N-oxide acts as a poor substrate for the P-glycoprotein (P-170) efflux pump. 10S,13aR-Antofine N-oxide can be used for the research of cancers.