Rhapontigenin is a selective inactivator of cytochrome P450 1A1 with IC50 of 400 nM. Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively. Rhapontigenin inhibits ADP- and collagen-induced platelet aggregation with IC50 values of 4 and 70 μg/ml, respectively. Rhapontigenin demonstrates a strong inhibitory activity on the 13-hexosaminidase release induced by DNP-BSA, it exhibits IC50 value of 0.03 mM in RBL 2H3 cells. In vivo, Rhapontigenin (25mg/kg; i.p.) shows significant protection from death due to pulmonary thrombosis in mice, those samples are orally administered 90 min before tail vein injection of epinephrine and collagen.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 60 mg/mL|
|Storage||2-8°C, protect from light, dry, sealed|
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