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Rhapontigenin

Cat. No. M9877
Rhapontigenin Structure
Synonym:

Protigenin

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 200  USD200 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 258.27
Formula C15H14O4
CAS Number 500-65-2
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage 2-8°C, protect from light, dry, sealed
References

[1] Yen-Hsiu Yeh, et al. Oncol Rep. Rhapontigenin inhibits TGF-β-mediated epithelial‑mesenchymal transition via the PI3K/AKT/mTOR pathway and is not associated with HIF-1α degradation

[2] Kathryn A Roupe, et al. J Pharm Pharm Sci. Preparative enzymatic synthesis and HPLC analysis of rhapontigenin: applications to metabolism, pharmacokinetics and anti-cancer studies

[3] Eun-Kyung Park, et al. Arch Pharm Res. Antithrombotic and antiallergic activities of rhaponticin from Rhei Rhizoma are activated by human intestinal bacteria

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Keywords: Rhapontigenin, Protigenin supplier, Cytochrome P450 (e.g. CYP17), inhibitors

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