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Bazedoxifene Acetate is a third generation, oral and nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 |
| Preparation method | For the proliferation assay, plating cells at 20,000 cells/well in a 24-well plate in DMEM/F12 (50:50) (phenol red-free) with 10% charcoal/dextran-treated FBS and 1 × GlutaMAX-1.Overnight incubation later, the medium is aspirated and treatments in DMEM/F12 (50:50) (phenol red-free) with 2% charcoal/dextran-treated FBS and 1 × GlutaMAX-1 are added to the wells. Each plate has a vehicle (baseline proliferation) and treatments. Treatments included 10 pM 17β-estradiol determined to be the EC80 for 17β-estradiol and 17β-estradiol in combination with six concentrations of BZA. Treatments from d 1 are renewed on d 3 and d 6 by aspirating medium from wells and replacing with fresh medium and treatments. On d 7, using trypsin-EDTA and counted using a Multisizer II to detach cell from the plate . |
| Concentrations | ~10 nM |
| Incubation time | 7 days |
| Animal Experiment | |
|---|---|
| Animal models | Sprague Dawley rats |
| Formulation | 50% dimethylsulfoxide-50% 1× Dulbecco’s PBS |
| Dosages | 0.5 and 5.0 mg/kg |
| Administration | SC |
| Molecular Weight | 530.65 |
| Formula | C30H34N2O3.C2H4O2 |
| CAS Number | 198481-33-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage | 4°C, protect from light, dry, sealed |
[1] No authors listed. Med Lett Drugs Ther. Drugs for postmenopausal osteoporosis
[2] No authors listed. Drug Ther Bull. Bazedoxifene for HRT?
[3] D Ashley Hill, et al. Hormone Therapy and Other Treatments for Symptoms of Menopause
[4] S Palacios. Bazedoxifene acetate for the management of postmenopausal osteoporosis
| Related Estrogen Receptor Products |
|---|
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GDC-0927 (SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist. |
| AC-186
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. |
| Idoxifene
Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM). |
| (R)-Equol
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively. |
| (Rac)-Vepdegestrant
(Rac)-Vepdegestrant is the isomer of Vepdegestrant. |
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