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 |
| 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.
[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 |
|---|
| hFSH-β-(33-53) TFA
hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells. |
| Yp537
Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor. |
| Palazestrant
Palazestrant is a novel, orally active, estrogen receptor antagonist and selective estrogen receptor degrader. It can be used in studies related to ER+/HER2+ breast cancer. |
| Acolbifene hydrochloride
Acolbifene hydrochloride is an active metabolite of EM800 and an orally available, selective estrogen receptor modulator (SERM) that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity, has significant anti-estrogenic effects on the mammary gland and uterus, and has anticancer activity. possesses anticancer activity. |
| Acolbifene
Acolbifene is an active metabolite of EM800 and an orally active pure anti-estrogen and selective estrogen receptor (ER) antagonist that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity and has anticancer activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
