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Bazedoxifene

Cat. No. M22417
Bazedoxifene Structure
Synonym:

TSE-424

Size Price Availability Quantity
5mg USD 99  USD99 In stock
10mg USD 148  USD148 In stock
25mg USD 295  USD295 In stock
50mg USD 440  USD440 In stock
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Quality Control & Documentation
Biological Activity

Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.

Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells. Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.

In vivo, Bazedoxifene (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model.

Chemical Information
Molecular Weight 470.6
Formula C30H34N2O3
CAS Number 198481-32-2
Form Solid
Solubility (25°C) DMSO 95 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Parth M. Raina, et al. Bazedoxifene

[2] Pengcheng Luo, et al. Eur J Pharmacol. Bazedoxifene exhibits anti-inflammation and anti-atherosclerotic effects via inhibition of IL-6/IL-6R/STAT3 signaling

[3] Maria P Yavropoulou, et al. Expert Opin Pharmacother. Bazedoxifene for the treatment of osteoporosis

[4] No authors listed. Aust Prescr. Conjugated oestrogens/bazedoxifene

[5] No authors listed. Drug Ther Bull. Bazedoxifene for HRT?

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Keywords: Bazedoxifene, TSE-424 supplier, Estrogen Receptor, inhibitors, activators


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