| 名稱 | Bazedoxifene hydrochloride |
| 描述 | Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6/GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases. |
| 細(xì)胞實(shí)驗(yàn) | For the proliferation assay, cells are plated at 20,000 cells/well in a 24-well plate in DMEM/F12 (50:50) (phenol red-free) with 10% charcoal/dextran-treated FBS and 1 × GlutaMAX-1. After overnight incubation, the medium is aspirated and treatments in DMEM/F12 (50:50) (phenol red-free) with 2% charcoal/dextran-treated FBS and 1 × GlutaMAX-1 are added to the wells. Each plate has a vehicle (baseline proliferation) and treatments. Treatments included 10 pM 17β-estradiol determined to be the EC80 for 17β-estradiol and 17β-estradiol in combination with six concentrations of BZA. Treatments from d 1 are renewed on d 3 and d 6 by aspirating medium from wells and replacing with fresh medium and treatments. On d 7, cells are detached from the plate using trypsin-EDTA and counted using a Multisizer II.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Ligand binding competition experiments: Test compounds are initially solubilized in DMSO and the final concentration of DMSO in the binding assay is ≤ 1%. Eight dilutions of each test compound are used as an unlabelled competitor for [3H]17β-estradiol. Typically, a set of compound dilutions would be tested simultaneously on human, rat and mouse ER-α and ER-β. The results are plotted as measured DPM vs. concentration of test compound. For dose-response curve fitting, a four parameter logistic model on the transformed, weighted data are fit and the IC50 is defined as the concentration of compound decreasing maximum [3H]estradiol binding by 50%. For active compounds, the IC50 is determined at least three times. It should be noted that IC50 values are not direct measures of a ligand's affinity for the receptor. Rather, they can only be compared as relative values, in this case to 17β-estradiol. |
| 體外活性 | 在 AsPC-1 細(xì)胞中，Bazedoxifene hydrochloride（10 μM-20 μM；2 小時(shí)）能夠抑制由 IL-6、IL-11 或 OSM（各50 ng/mL）誘導(dǎo)的 STAT3 磷酸化[2]。 |
| 體內(nèi)活性 | 在 6 周齡的雌性無胸腺裸鼠中，Bazedoxifene hydrochloride（劑量為5 mg/kg；通過口服灌胃，每日一次，持續(xù) 18 天）被用于抑制胰腺癌異種移植瘤的生長(zhǎng)，并在腫瘤細(xì)胞中誘導(dǎo)凋亡[2]。 |
| 存儲(chǔ)條件 | Store at low temperature,Keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : <1 mg/mL
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (19.72 mM), Solution.
10% DMSO+90% Saline : < 10 mg/mL (19.72 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
Ethanol : <1 mg/mL
DMSO : 125 mg/mL (246.52 mM), Sonication is recommended.
|
| 關(guān)鍵字 | TSE-424 | TSE424 | TSE 424 | STAT3 | SERM | selective | receptor | protein-protein | progestogenReceptor | progestogen Receptor | modulator | interactions | ILReceptor | IL-6/GP130 | IL-6 | IL Receptor | GP130 | EstrogenReceptor | Estrogen Receptor/ERR | Estrogen Receptor | estrogen | ERβ | ERα | ERR | Bazedoxifene HCl | Bazedoxifene |
| 相關(guān)產(chǎn)品 | Cholesterol | Rhamnose monohydrate | Kaolin | 1-Tetradecanol | Tributyrin | Gluconate Calcium | Tamoxifen | Gluconate sodium | 1,8-Cineole | Triphenyl phosphate | D(+)-Raffinose pentahydrate | Hydroxypropyl Cellulose |
| 相關(guān)庫 | 抑制劑庫 | 抗癌上市藥物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 上市藥物庫 | FDA 上市藥物庫 | 核受體化合物庫 | 免疫/炎癥分子化合物庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 | PPI抑制劑庫 | 抗癌藥物庫 |