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Bazedoxifene acetate (Synonyms: TSE-424 acetate)

製品番号: HY-A0036 純度: 99.88%
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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用としては使用しないように、十分ご注意ください。

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 (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 98 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 84 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 144 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 432 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 660 在庫あり
Estimated Time of Arrival: December 31
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

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of Bazedoxifene acetate:

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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].

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].

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

198481-33-3

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, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (188.45 mM)

H2O : 1 mg/mL (1.88 mM; Need ultrasonic)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献

純度: 99.88%

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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

Keywords:

BazedoxifeneTSE-424TSE424TSE 424Estrogen Receptor/ERRselectiveestrogenreceptormodulatorSERMERαERβIL-6/GP130protein-proteininteractionsSTAT3Inhibitorinhibitorinhibit

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