GNE-7915 NEW
| Price | $34 | $70 | $118 |
| Package | 10mg | 25mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-04 |
Product Details
| Product Name: GNE-7915 | CAS No.: 1351761-44-8 |
| Purity: ≥95% | Supply Ability: 10g |
| Release date: 2024/11/04 |
Product Introduction
Bioactivity
| 名稱(chēng) | GNE-7915 |
| 描述 | GNE-7915 is a highly potent, selective and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor. |
| 激酶實(shí)驗(yàn) | ALK2 kinase assay: Puri?ed recombinant ALK2 proteins, ATP, ATP[γ-32P], and dephosphorylated casein at ?nal concentrations of 2.5 nM, 6 μM, 0.05 μCi/μL , and 0.5 mg/mL, respectively, are aliquoted in kinase bu?er containing 0.2% BSA supplemented with 10 mM MnCl2 into 96-microwell plates, in combination with inhibitor compounds diluted at varying concentrations (0.01 nM to 100 μM). Positive control samples lacking inhibitor compounds, and negative controls lacking recombinant kinase, are also measured. The mixture is reacted at RT for 45 min, quenched with a ?nal concentration of 2% phosphoric acid. The reaction mixture is transferred to 96-well P81 phosphocellulose ?lter plates and bound for 5 min. The plates are washed 20 times with 150 μL of 1% phosphoric acid solution per well by vacuum manifold. Plates are dried at RT for 1 h, sealed, and assayed with Microscint 20 scintillation ?uid using a Spectramax L luminometer. Data is normalized to positive controls at 100% enzyme activity, with negative controls being subtracted as background. |
| 體外活性 | BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson's disease mutation (PD mutation), exhibit concentration-dependent gene silencing of pLRRK2 in the brain following intraperitoneal injection or oral administration of 50 mg/kg GNE-7915. In rats, GNE-7915 demonstrates favorable pharmacokinetic (PK) properties, including a long half-life, good oral bioavailability, and high passive permeability. |
| 體內(nèi)活性 | GNE-7915 exhibits excellent in vitro pharmacokinetics in human hepatocytes with minimal conversion rates. According to in vitro functional assays, GNE-7915 also acts as a moderately effective antagonist of 5-HT2B. |
| 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 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 16.67 mg/mL (37.59 mM), Sonication is recommended. |
| 關(guān)鍵字 | LRRK2 | inhibit | Inhibitor | GNE 7915 | Leucine-rich repeat kinase 2 | GNE-7915 |
| 相關(guān)產(chǎn)品 | PFE-360 | GNE0877 | CZC-25146 | GSK2578215A | GNE-9605 | CZC-54252 hydrochloride | EB-42486 | LRRK2 inhibitor 1 | LRRK2-IN-7 | LRRK2-IN-1 | CCG-1423 | PF-06454589 |
| 相關(guān)庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 谷氨酰胺代謝化合物庫(kù) | 抗帕金森病化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 抗衰老化合物庫(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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United States- Since: 2011-01-07
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