Bazedoxifene acetate

• CAS: 198481-33-3
• Catalog Number: ACM198481333
• Category: Others
• Molecular Weight: 530.67
• Molecular Formula: C32H38N2O5
• Description: Bazedoxifene, also known as WAY-140424, is a third generation selective estrogen receptor modulator (SERM), developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. In late 2013, Pfizer received approval for bazedoxifene as part of the combination drug DUAVEE in the prevention (not treatment) of postmenopausal osteoporosis. Bazedoxifene is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).
• Synonyms: Bazedoxifene acetate, WAY-140424; WAY140424; WAY 140424; TSE 424; TSE424; TSE-424; Viviant
• IUPAC Name: 1-(p-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)benzyl)-2-(p-hydroxyphenyl)-3-methylindol-5-ol acetic acid
• Canonical SMILES: OC1=CC2=C(C=C1)N(C(C3=CC=C(C=C3)O)=C2C)CC4=CC=C(C=C4)OCCN5CCCCCC5.CC(O)=O
• InChI: InChI=1S/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)
• InChI Key: OMZAMQFQZMUNTP-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Alternative CAS: 198481-32-2 (free base); 198480-56-7 (HCl); 198481-33-3 (acetate)
• Biological Target: Bazedoxifene acetate is a selective estrogen receptor modulator (SERM) with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 72.43; H, 7.22; N, 5.28; O, 15.07
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: The purpose of this study was to investigate the effects of Bazedoxifene on the functional changes of vascular smooth muscle cells (VSMCs) after PDGF-BB stimulation. PDGF-BB treatment significantly enhanced the viability and proliferation of VSMCs as indicated by CCK-8 and EdU assays (P < 0.01), while Bazedoxifene pretreatment could reduce the increased viability and proliferation of VSMCs caused by PDGF-BB (P < 0.05). Wound healing test also showed Bazedoxifene significantly attenuated the migration in the PDGF-BB stimulated VSMCs (P < 0.01). PDGF-BB also induced the phenotypic switch and decreased the autophagy level in VSMCs, manifested as a reduction in vimentin, SMA, and LC3 II (P < 0.01). These effects of PDGF-BB were partially reversed by Bazedoxifene (P < 0.05). These results indicated that Bazedoxifene may inhibit the proliferation and migration of VSMCs through up-regulate the autophagy level after PDGF-BB stimulation.; Reference: Life Sci. 2020 Oct 15;259:118397. https://www.sciencedirect.com/science/article/abs/pii/S0024320520311504?via%3Dihub
• In Vivo Activity: The effect of Bazedoxifene in the progression of atherosclerosis was evaluated in apolipoprotein E-deficient (ApoE-/-) mice. Five-week-old male ApoE-/- mice were fed with High-fat diet (HFD) containing 5 mg/kg Bazedoxifene or a matching control for 12 weeks. Oil red O (ORO) staining was used to detect plaque size; immunohistochemical staining was used to detect the presence of endothelial cells, vascular muscle cells and phosphorylated STAT3 (P-STAT3) in localized plaques. The potential underlying mechanisms in human umbilical vein endothelial cells (HUVECs) and vascular muscle cells (VSMCs) was detected by Western blot analysis, Wound healing assay and Elisa assay. In the ApoE-/- mice fed with HFD, daily Bazedoxifene administration effectively attenuated atherosclerotic plaque area (P < 0.01), down-regulated IL-6 levels (P < 0.01), decreased STAT3 phosphorylation, reduced VSMCs proliferation and increased endothelial coverage in aortic vessels. Bazedoxifene did not inhibit the growth of HUVECs while suppressing the proliferation of VSMCs.; Reference: Eur J Pharmacol. 2021 Feb 15;893:173822. https://www.sciencedirect.com/science/article/abs/pii/S0014299920309274?via%3Dihub
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).