MK-0752 NEW
| Price | $52 | $163 | $255 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: MK-0752 | CAS No.: 471905-41-6 |
| Purity: 99.55% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名称 | MK-0752 |
| 描述 | MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM). |
| 激酶实验 | Protein kinase assays : Protein kinase assays are either done in-house by ELISA-based assay methods (Kit, KDR, PDGFRα, and PDGFRβ) or by a radiometric method. In-house ELISA assays used poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates; phosphorylation is then detected using an antiphosphotyrosine antibody conjugated to HRP. The bound antibody is then quantitated using ABTS as the peroxidase substrate by measuring the absorbance at 405/490 nm. All assays uses purified recombinant kinase catalytic domains that are either expressed in insect cells or in bacteria. The Kit and EGFR protein used for in-house assays are prepared internally; other enzymes are obtained. Recombinant Kit protein is expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and is initially purified as a nonphosphorylated (nonactivated) enzyme with a relatively high Km for ATP (400 μM). In some assays, an activated (tyrosine phosphorylated) form of the enzyme is prepared by incubation with 1 mM ATP for 1 hour at 30 °C. The phosphorylated protein is then passed through a desalting column to remove the majority of the ATP and stored at ?80 °C in buffer containing 50% glycerol. The resultant preparation has a considerably higher specific activity and a lower Km for ATP (25 μM) than the initial nonphosphorylated preparation. The inhibition of Kit autophosphorylation by OSI-930 is assayed by incubation of the nonphosphorylated enzyme at 30 °C in the presence of 200 μM ATP and various concentrations of OSI-930. The reaction is stopped by removal of aliquots into SDS-PAGE sample buffer followed by heating to 100 °C for 5 minutes. The degree of phosphorylation of Kit is then determined by immunoblotting for both total Kit and phosphorylated Kit. |
| 体外活性 | In guinea pigs, oral administration of MK-0752 (10-30 mg/kg) resulted in a dose-dependent reduction of Aβ40 in the plasma, brain, and cerebrospinal fluid. Similarly, in monkeys, MK-0752 (240 mg/kg) was capable of reducing the production of Aβ in the brain. |
| 体内活性 | In human SH-SY5Y cells, MK-0752 significantly reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM. |
| 存储条件 | 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) DMSO : 89 mg/mL (200.94 mM) Ethanol : 45 mg/mL (101.6 mM) |
| 关键字 | Aβ40 | inhibit | barrier | γ-secretase | blood-brain | Inhibitor | MK 0752 | CNS | MK0752 | MK-0752 | Gamma secretase |
| 相关产品 | Anle138b | Notoginsenoside R1 | Geniposide | Deferoxamine Mesylate | Valproic acid sodium salt | Tramiprosate | Dihydroergocristine mesylate | Rutin | Valproic Acid | CB-103 | Carvacrol | Methyl tridecanoate |
| 相关库 | 经典已知活性库 | 神经退行性疾病化合物库 | 儿童药物库 | ReFRAME 相关化合物库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
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
- Address: 36 Washington Street, Wellesley Hills
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