Biological Activity
HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.
In Vitro
Compared with control (0 nM HM30181A), paclitaxel potently inhibits the survival of K1735 cells by about 65% at 100 nM and 72% at 1000 nM in a dose-dependent manner. HM30181A does not make any significant changes in the survival of K1735 cells. In contrast, bEnd.3 cells do not show any decreases in survival by the paclitaxel treatment without HM30181A. However, treatment of 0.1 or 1 nM HM30181A lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM paclitaxel treatment, respectively[2].
In Vivo
The plasma concentrations of HM30181M are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h (p < 0.05). The microcapsule has about a 1.7-fold faster Tmax and a 1.6-fold higher AUC value compared with the powder (2.5±0.6 vs. 4.3±0.9 h; 107.7±20.1 vs. 64.3±18.0 h ng/mL). The faster and overall improved absorption of HM30181M in microcapsule form might be due to the remarkable enhancement of the aqueous solubility and dissolution resulting from its crystalline conversion to the amorphous form and particle size reduction[1].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.