Transport experiments with Caco-2 cells show that 6-Methylcoumarin presents high permeability at all concentrations evaluated. This finding suggests that 6-Methylcoumarin could be transported across the gut wall by passive diffusion.
The plasma concentration-time curve shows that the maximum concentration (Cmax) is 17.13 ± 2.90 µg/mL at maximum time (Tmax) of 30 min for the oral route (200 mg/kg) and Cmax 26.18 ± 2.47 µg/mL at 6.0 min for the intraperitoneal administration (200 mg/kg), with elimination constant of (Ke) 0.0070/min and a short life half time of (T1/2) lower that 120 min. 6-Methylcoumarin has high accumulation in the liver, and widespread distribution in all the organs evaluated. The oral bioavailability (F) of 6-Methylcoumarin is 45% in Wistar rats.
Molecular Weight | 160.17 |
Formula | C10H8O2 |
CAS Number | 92-48-8 |
Solubility (25°C) | DMSO: ≥ 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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