AZD 4017 NEW
Price | $67 | $163 | $289 |
Package | 1mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-01 |
Product Details
Product Name: AZD 4017 | CAS No.: 1024033-43-9 |
Purity: 99.39% | Supply Ability: 10g |
Release date: 2024/11/01 |
Product Introduction
Bioactivity
名稱(chēng) | AZD 4017 |
描述 | AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM). |
體外活性 | AZD 4017 exhibits significant inhibition of a crucial target tissue (IC50=0.002 μM), aligning well with its enzyme potency, suggesting its effectiveness in adipose tissue is not compromised by its acidic nature[1]. It demonstrates remarkable selectivity against related enzymes 11-βHSD2, 17β-HSD1, and 17β-HSD3 (all IC50>30 μM), while showing negligible activity towards glucocorticoid and mineralocorticoid receptors. Although AZD 4017 is highly potent against the human variant of 11β-HSD1, its efficacy significantly diminishes across species, excluding cynomolgous monkey (IC50=0.029 μM). Considering adipose tissue as a critical organ, the compound's ability to inhibit 11β-HSD1 activity has been confirmed in isolated human adipocytes from nondiabetic volunteers. |
體內(nèi)活性 | AZD 4017 exhibits dose-dependent inhibition of 11β-HSD1, with its effect being limited by lower potency against the mouse enzyme, restricting the scope of preclinical pharmacodynamic measurements. Increasing doses achieved a peak inhibition of roughly 70% at 1500 mg/kg, corresponding to 10×IC50 in mice, demonstrating the compound's efficacy in this model[1]. |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 125 mg/mL (297.92 mM) |
關(guān)鍵字 | AZD4017 | inhibit | AZD-4017 | Inhibitor | AZD 4017 |
相關(guān)產(chǎn)品 | Disulfiram | Methotrexate | ALDH1A3-IN-3 | Rotenone | Mycophenolate Mofetil | Ribavirin | 4-Diethylaminobenzaldehyde | Benzyl alcohol | Isomalt | Isoniazid | Sodium Oxamate | Ivosidenib |
相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | ReFRAME 相關(guān)化合物庫(kù) | 抗癌細(xì)胞代謝庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | 代謝化合物庫(kù) | 臨床期小分子藥物庫(kù) | 已知活性化合物庫(kù) |
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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