| Description | 6-Methylcoumarin (Toncarine) (6MC) is a semisynthetic coumarin with important in vitro and in vivo anti-inflammatory activity. |
| In vitro | 通过与Caco-2细胞的运输实验表明，在所有评估的浓度下，6MC展现了高渗透性。这暗示6MC可能通过被动扩散过程跨越肠壁运输。 |
| In vivo | 6-Methylcoumarin（6MC）可通过被动扩散过程跨越肠壁。口服途径时，最大浓度（Cmax）为17.13 ± 2.90 μg/mL，达到最大浓度的时间（Tmax）为30分钟；而通过腹膜内给药时，Cmax为26.18 ± 2.47 μg/mL，达到最大浓度的时间为6.0分钟。6MC的消除常数（Ke）为0.0070 min^-1，半衰期（T1/2）小于120分钟。6MC在肝脏中高度积累，并在所评估的所有器官中广泛分布。 |
| Cell experiments | The determination of in vitro intestinal permeability of 6MC was carried out under sink conditions in a series of pH-gradient bidirectional transport experiments with Caco-2 cells. Before the experiments, cell monolayers were rinsed with Hank's balanced salt solution (HBSS) and equilibrated for 30 min at 37 °C. The integrity of the monolayers was assessed before and after the experiments, by transepithelial electrical resistance (TEER) measurement. Only monolayers with TEER values above 200 Ωcm2 were considered. A stock solution of 6MC (10 mM DMSO) was diluted to final concentration of 10, 25, 50 or 100 μM in HBSS pH 6.5 (apical transport buffer) or pH 7.4 (basolateral transport buffer). Bidirectional experiments (apical-to-basolateral [AB] and basolateral-to-apical [BA]) were initiated by adding 6MC solutions to the donor compartment, and fresh buffer to the acceptor compartment. Caco-2 cell monolayers were incubated for 1 h at 37 °C under constant stirring (150 rpm). Receiver compartments were sampled at 0, 15, 30, 45 and 60 min, refilled with an equivalent amount of transport buffer, and samples were submitted to analysis by HPLC/UV. |
| Synonyms | Toncarine, 6-甲基香豆素 |
| molecular weight | 160.17 |
| Molecular formula | C10H8O2 |
| CAS | 92-48-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 55 mg/mL (343.39 mM) |
| References | 1. Cárdenas Paola Andrea, Kratz Jadel Müller, Hernández Aura, et al. In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats[J]. Brazilian Journal of Pharmaceutical Sciences, 2017, 53(1). |