Avagacestat NEW
Price | $57 | $123 | $237 |
Package | 1mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-16 |
Product Details
Product Name: Avagacestat | CAS No.: 1146699-66-2 |
Purity: 99.77% | Supply Ability: 10g |
Release date: 2024/11/16 |
Product Introduction
Bioactivity
名稱 | Avagacestat |
描述 | Avagacestat (BMS-708163) (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2. |
細(xì)胞實(shí)驗(yàn) | BMS-708163 is dissolved in DMSO. The cell viability is assessed using a tetrazolium salt (WST-8)-based colorimetric assay from the Cell Counting Kit 8 (CCK-8). The cells are seeded into 96-well plates at an initial density of 5×103 cells/well and cultured for 24?h, after which the cells are cultured with DMSO, increased concentrations of gefitinib or BMS708163, BIBW2992, or the combination of BMS708163 and BIBW2992 for an additional 48?h. The A450 is measured in a microplate reader after 10?μL of CCK-8 solution is added and incubated for 1?h. The percentage of growth is shown relative to untreated controls. |
體外活性 | BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. [1] |
體內(nèi)活性 | Oral administration of BMS-708163 significantly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs. BMS-708163 has no dose-limiting effects in dogs (3 mg/kg during 6 months), with a high brain to plasma ratio (2.4). [1] |
存儲(chǔ)條件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 96 mg/mL (184.3 mM) |
關(guān)鍵字 | Inhibitor | γ-secretase | Avagacestat | Notch | BMS708163 | Gamma secretase | BMS 708163 | inhibit |
相關(guān)產(chǎn)品 | Valproic acid sodium salt | Aβ42-IN-2 | Tangeretin | gamma-secretase modulator 1 | FLI-06 | Valproic Acid | CB-103 | Gossypolone | IMR-1A | Carvacrol | RO7185876 | DAPT |
相關(guān)庫 | 表型篩選靶點(diǎn)鑒定庫 | 經(jīng)典已知活性庫 | 神經(jīng)退行性疾病化合物庫 | 抗阿爾茨海默癥化合物庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 |
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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