Ro 48-8071 fumarate NEW
| Price | $45 | $68 | $207 |
| Package | 5mg | 10mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-07 |
Product Details
| Product Name: Ro 48-8071 fumarate | CAS No.: 189197-69-1 |
| Purity: 99.32% | Supply Ability: 10g |
| Release date: 2024/11/07 |
Product Introduction
Bioactivity
| 名稱 | Ro 48-8071 fumarate |
| 描述 | Ro 48-8071 fumarate, an inhibitor of OSC (Oxidosqualene cyclase; IC50=6.5 nM), exhibits LDL (low-density lipoprotein) cholesterol-lowering activity. |
| 體外活性 | Ro 48-8071 reduces cholesterol synthesis dose-dependently with an IC50 value of appr 1.5 nM in HepG2 cells[1]. Ro 48-8071 (10 μM) significantly reduces the viability of PC-3 prostate cancer cells, but not normal prostate cells. Ro 48-8071 (10-30 μM) induces apoptosis of both LNCaP and C4-2 cell lines in a dose-dependent manner. And castration-resistant PC-3 and DU145 cells also demonstrate significant levels of apoptosis following 24-hour treatment with Ro 48-8071. Ro 48-8071 (10-25 μM) reduces AR protein expression in a dose-dependent manner. Ro 48-8071 (0.1-1 μM) increases ERβ protein expression dose-dependently in both hormone-dependent LNCaP and castration-resistant PC-3 cells[2]. Using mammalian cells engineered to express human ERα or ERβ protein, together with an ER-responsive luciferase promoter, Ro 48-8071 dose-dependently inhibits 17β-estradiol (E2)-induced ERα responsive luciferase activity (IC50, appr 10 μM), under conditions that are non-toxic to the cells[3]. |
| 體內(nèi)活性 | Ro 48-8071 effectively reduces LDL-C by approximately 60% at a dose of 150 μmol/kg per day without further decrease at up to 300 μmol/kg per day, while not affecting HDL-C levels at any dose in hamsters. At doses of 300 μmol/kg per day or higher, it significantly elevates MOS levels in the liver and markedly diminishes VLDL secretion in hamsters. Additionally, Ro 48-8071, at 5 or 20 mg/kg, substantially curtails in vivo tumor growth in mice and completely eliminates two out of 12 monitored tumors at 20 mg/kg, without causing weight loss in the mice. Furthermore, at 20 mg/kg/day, it achieves a rapid and enduring suppression of more than 50% in cholesterol synthesis in the entire small intestine of BALB/c mice, along with reductions in sterol synthesis in the large intestine and stomach. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 22.5 mg/mL (39.86 mM) |
| 關(guān)鍵字 | Ro 48-8071 Fumarate | Ro 488071 fumarate | Ro 48 8071 fumarate | Ro 48-8071 | Inhibitor | inhibit |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抑制劑庫 | 抗心血管疾病化合物庫 | NO PAINS 化合物庫 | 已知活性化合物庫 | 活性脂質(zhì)化合物庫 | 含氟化合物庫 | 抗COVID-19化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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