Name | Bazedoxifene Acetate |
Synonyms | Viviant Way-140424 WAY-140424 UNII-J70472UD3D Unii-J70472ud3d BAZEDOXIFENE ACETATE Bazedoxifene Acetate Bazedoxifene acetate [usan] 1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate 1-(p-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)benzyl)-2-(p-hydroxyphenyl)-3-methylindol-5-ol monoacetate (salt) 1-((4-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol monoacetate 1H-Indol-5-ol, 1-((4-(2-(hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-, monoacetate (salt) |
CAS | 198481-33-3 |
EINECS | 638-804-4 |
InChI | InChI=1/C30H34N2O3.C2H4O2/c1-22-28-20-26(34)12-15-29(28)32(30(22)24-8-10-25(33)11-9-24)21-23-6-13-27(14-7-23)35-19-18-31-16-4-2-3-5-17-31;1-2(3)4/h6-15,20,33-34H,2-5,16-19,21H2,1H3;1H3,(H,3,4) |
InChIKey | DGEPGJZKMFNSDD-UHFFFAOYSA-N |
Molecular Formula | C30H34N2O3.C2H4O2 |
Molar Mass | 530.661 |
Melting Point | 174-178° |
Boling Point | 694.4°C at 760 mmHg |
Flash Point | 373.8°C |
Solubility | DMSO: soluble15mg/mL, clear |
Vapor Presure | 6.33E-20mmHg at 25°C |
Appearance | powder |
Color | white to beige |
Storage Condition | -20°C |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.884 ml | 9.422 ml | 18.845 ml |
5 mM | 0.377 ml | 1.884 ml | 3.769 ml |
10 mM | 0.188 ml | 0.942 ml | 1.884 ml |
5 mM | 0.038 ml | 0.188 ml | 0.377 ml |
mechanism of action | the mechanism of action of badoxifene acetate is unique and is a new type of selective estrogen receptor modulator (SERM), which has a selective regulatory effect on estrogen receptor. Bardoxifene has estrogen receptor agonism in certain tissues of the body, and has the same effect as estrogen in human bones (estrogen can delay bone aging and reduce fracture occurrence). |
Use | Baxifene acetate is a non-steroidal selective estrogen receptor modulator (SERM). Baxifene acetate is used to fight osteoporosis. |
biological activity | Bazedoxifene acetate (TSE-424 acetate) is an orally active, non-steroidal, selective estrogen receptor modulator (SERM). The IC50 values for ERα and ERβ are 26 nM and 99 nM respectively, which can be used for the study of osteoporosis. Bazedoxifene acetate is also a IL-6/GP130 protein interaction inhibitor, which can be used for pancreatic cancer research. |
target | IC50: 26 nM (ERα), 99 nM (ERβ) |
Cell Line: | AsPC-1 cells Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells |
Concentration: | 10 μM, 20 μM 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: | 2 hours Overnight |
Result: | Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation. Induced apoptosis. Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells. |
Animal Model: | 6-week-old female athymic nude mice |
Dosage: | 5 mg/kg |
Administration: | Oral gavage, daily, for 18 days |