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.
Molecular Weight | 258.27 |
Formula | C15H14O4 |
CAS Number | 500-65-2 |
Solubility (25°C) | DMSO ≥ 60 mg/mL |
Storage | 2-8°C, protect from light, dry, sealed |
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.
Related Cytochrome P450 (e.g. CYP17) Products |
---|
Cytochrome P450 reductase
Cytochrome P450 reductase is a NADPH-cytochrome reductase. |
20-SOLA
20-SOLA is a water-soluble 20-HETE antagonist. |
TS-011
TS-011 is a selective inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis. |
Dibromo-dodecenyl-methylsulfimide
Dibromo-dodecenyl-methylsulfimide is a selective inhibitor of 20-HETE synthesis and attenuates the vasodilatory response to sodium nitroprusside (SNP). |
Abiraterone decanoate
Abiraterone decanoate is a novel, long-acting Abiraterone precursor compound that also exhibits high CYP17 cleavage enzyme inhibition selectivity for prostate cancer related studies. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.