Home>>Signaling Pathways>> Others>> Estrogen Receptor/ERR>>Bazedoxifene

Bazedoxifene

Catalog No.GC14883

Products are for research use only. Not for human use. We do not sell to patients.

Bazedoxifene Chemical Structure

Cas No.: 198481-32-2

Size Price Stock Qty
5mg
$81.00
In stock
10mg
$146.00
In stock
25mg Please Inquire Please Inquire
50mg Please Inquire Please Inquire

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Background

Bazedoxifene is a selective estrogen receptor modulator (SERM) with IC50 value of 26 and 99 nM for estrogen receptorα and β, respectively [1].
Bazedoxifene is a SERM used for the prevention and treatment of post menopausalo steoporosis which is caused by the loss of endogenous levels of estrogens. It is developed as a third-generation SERM which can reduce the vertebral and nonvertebral fracture risk and have no stimulatory effects on breast or uterus. Bazedoxifene is an estrogen receptor ligand with an indole-based core binding domain. It binds to both ERα (IC50 value of 23nM) and ERβ (IC50 value of 85nM), exhibited agonist activity in bone, cardiovascular system and CNS while exhibited antagonist activity in breast and endometrium. It competitively inhibited the binding of 17β-estradiol to both ERα and ERβ [1, 2 and 3].
In MCF7 cells, treatment of bazedoxifene showed no ER agonist activity and no effect on the cell proliferation. However, it suppressed the 17β-estradiol -induced transcriptional activation and cell proliferation [3].
In ovariectomized rats, administration of bazedoxifene at dose of 0.3 or 3.0 mg /kg daily for 6 weeks resulted in the protection of skeleton from bone loss with increased bone mineraldensity. In addition, the compression strength of the fifth lumbar vertebra was significantly improved by bazedoxifene. Moreover, administration of bazedoxifene at dose of3.0 mg /kg/day showed modest stimulatory effects on rat uterine with small increase in wet uterine weight. Bazedoxifene also had no ER agonist effects on rat vasomotor activity [2 and 3].
References:
[1] de Villiers TJ. Bazedoxifene: a novel selective estrogen receptor modulator for postmenopausal osteoporosis. Climacteric. 2010 Jun;13(3):210-8.
[2] Duggan ST, McKeage K. Bazedoxifene: a review of its use in the treatment of postmenopausal osteoporosis. Drugs. 2011 Nov 12;71(16):2193-212.
[3] Kawate H, Takayanagi R. Efficacy and safety of bazedoxifene for postmenopausal osteoporosis. Clin Interv Aging. 2011;6:151-60.

Chemical Properties

Cas No. 198481-32-2 SDF
Chemical Name 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol
Canonical SMILES CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O
Formula C30H34N2O3 M.Wt 470.6
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1249 mL 10.6247 mL 21.2495 mL
5 mM 0.425 mL 2.1249 mL 4.2499 mL
10 mM 0.2125 mL 1.0625 mL 2.1249 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for Bazedoxifene

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Bazedoxifene

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.