(1S,2R)-Alicapistat NEW
| Price | $147 | $367 | $521 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-12 |
Product Details
| Product Name: (1S,2R)-Alicapistat | CAS No.: 2221010-57-5 |
| Purity: 98.05% | Supply Ability: 10g |
| Release date: 2024/11/12 |
Product Introduction
Bioactivity
| 名稱 | (1S,2R)-Alicapistat |
| 描述 | (1S,2R)-Alicapistat ((1S,2R)-ABT-957) is a highly efficient, orally active compound that selectively inhibits human calpains 1 and 2, showing promise for Alzheimer's disease (AD) therapy [1]. It effectively addresses the metabolic liability associated with carbonyl reduction and demonstrates potent inhibition of calpain 1 with an IC50 value of 395 nM [2]. |
| 體外活性 | (1S,2R)-Alicapistat fails to achieve sufficient concentrations in the central nervous system (CNS) for a pharmacodynamic effect [1]. It inhibits Calpain 1 (μ-calpain) and 2 (m-calpain) in a calcium-dependent manner, requiring μ-molar or m-molar calcium concentrations for activation. At 100 nM, (1S,2R)-Alicapistat (compound 22) prevents deficits in synaptic transmission caused by Aβ oligomer in rats [2]. Furthermore, at 385 nM, it effectively prevents NMDA-induced neurodegeneration and amyloid beta (Aβ)-induced synaptic dysfunction [2]. At concentrations ranging from 9-21 nM in cerebrospinal fluid (CSF), (1S,2R)-Alicapistat does not reach the IC 50 required for calpain inhibition, yet it exhibits no dose-limiting toxicities (DLTs) across broad population studies [3]. |
| 體內(nèi)活性 | '(1S,2R)-Alicapistat (compound 22), administered intravenously (iv) or orally (po) at doses of 1-3 mg/kg, shows moderate plasma clearance rates (CLp) in mouse, rat, and dog (0.13-1.04 L/hr.kg) and higher rates in monkeys (1.98 L/hr.kg). The average steady-state volume of distribution (Vss) is moderate in mouse, dog, and monkey (0.64-1.8 L/kg), with rats displaying higher values (3.4 L/kg). The plasma elimination half-life (t 1/2) varies, being shortest in dogs (1.7 hours), 2.3 hours in monkeys, and approximately 6.0 hours in mice and rats. Oral bioavailability (F) is high in mice, rats, and dogs (>80%) but moderate in monkeys (14%) [2].' |
| 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 : 45 mg/mL (103.81 mM), Sonication is recommended. |
| 關(guān)鍵字 | Alicapistat | (1S,2R)Alicapistat |
| 相關(guān)產(chǎn)品 | Papain | 2-Aminoethanethiol | (S)-(+)-Ibuprofen | PMSF | KGP94 | N-Ethylmaleimide | Z-Lys-OH | Leupeptin Hemisulfate | 2-Cyanopyrimidine | Esomeprazole | Aloxistatin | E-64 |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抑制劑庫(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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United States- Since: 2011-01-07
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