1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. Bazedoxifene acetate

Bazedoxifene acetate  (Synonyms: TSE-424 acetate)

製品番号: HY-A0036 純度: 99.98%
COA 取扱説明書

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

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Bazedoxifene acetate 構造式

Bazedoxifene acetate 構造式

CAS 番号 : 198481-33-3

容量 価格(税別) 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 58 在庫あり
Solution
10 mM * 1 mL in DMSO USD 58 在庫あり
Solid
5 mg USD 50 在庫あり
10 mg USD 70 在庫あり
50 mg USD 140 在庫あり
100 mg USD 200 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Other Forms of Bazedoxifene acetate:

Top Publications Citing Use of Products

Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].

IC50 & Target

IC50: 26 nM (ERα), 99 nM (ERβ)[1]

体外実験

Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].
? Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling[1].
? Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells[2].
? Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].
? Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6[2].
? Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: AsPC-1 cells
Concentration: 10 μM, 20 μM
Incubation Time: 2 hours
Result: Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation.

Apoptosis Analysis[2]

Cell Line: Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells
Concentration: 10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC)
Incubation Time: Overnight
Result: Induced apoptosis.
体内実験

Bazedoxifene acetate (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week-old female athymic nude mice[2]
Dosage: 5 mg/kg
Administration: Oral gavage, daily, for 18 days
Result: Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.
臨床実験
分子量

530.65

分子式

C32H38N2O5

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C2=CC=C(O)C=C2)N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C5=CC=C(O)C=C51.CC(O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (188.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8845 mL 9.4224 mL 18.8448 mL
5 mM 0.3769 mL 1.8845 mL 3.7690 mL
10 mM 0.1884 mL 0.9422 mL 1.8845 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.75 mg/mL (5.18 mM); Clear solution

  • Protocol 2

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (5.18 mM); Clear solution

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.98%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8845 mL 9.4224 mL 18.8448 mL 47.1120 mL
5 mM 0.3769 mL 1.8845 mL 3.7690 mL 9.4224 mL
10 mM 0.1884 mL 0.9422 mL 1.8845 mL 4.7112 mL
15 mM 0.1256 mL 0.6282 mL 1.2563 mL 3.1408 mL
20 mM 0.0942 mL 0.4711 mL 0.9422 mL 2.3556 mL
25 mM 0.0754 mL 0.3769 mL 0.7538 mL 1.8845 mL
30 mM 0.0628 mL 0.3141 mL 0.6282 mL 1.5704 mL
40 mM 0.0471 mL 0.2356 mL 0.4711 mL 1.1778 mL
50 mM 0.0377 mL 0.1884 mL 0.3769 mL 0.9422 mL
60 mM 0.0314 mL 0.1570 mL 0.3141 mL 0.7852 mL
80 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5889 mL
100 mM 0.0188 mL 0.0942 mL 0.1884 mL 0.4711 mL
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Bazedoxifene acetate Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Bazedoxifene acetate
製品番号:
HY-A0036
数量:
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