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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Proteases>Gamma-secretase inhibitors>Avagacestat
Avagacestat
  • Avagacestat

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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