Lumacaftor NEW
| Price | $43 | $61 | $75 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-07 |
Product Details
| Product Name: Lumacaftor | CAS No.: 936727-05-8 |
| Purity: 99.72% | Supply Ability: 10g |
| Release date: 2024/11/07 |
Product Introduction
Bioactivity
| 名稱 | Lumacaftor |
| 描述 | Lumacaftor (VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM). |
| 細(xì)胞實(shí)驗(yàn) | FRT, HEK-293, or HBE cells expressing CFTR or F508del-CFTR were incubated for 24 h at 37 °C with or without VX-809 in the assay media. After incubation, cells were harvested in ice-cold D-PBS solution (without calcium and magnesium) and pelleted at 1,000 × g at 4 °C. Cell pellets were lysed in 1% Nonidet P-40, 0.5% sodium deoxycholate, 200 mM NaCl, 10 mM Tris, pH 7.8, and 1 mM EDTA plus protease inhibitor mixture (1:250) for 30 min on ice. Lysates were spun for 10 min at 10,000 × g at 4 °C to pellet nuclei and insoluble material. Approximately 12 μg total protein was heated in Laemmli buffer with 5% β-mercaptoethanol at 37 °C for 5 min and loaded onto a 3% to 8% Tris-acetate gel. The gel was transferred to nitrocellulose and processed for Western blotting by using monoclonal CFTR antibody 769 or polyclonal to GAPDH. Blots were developed by enhanced chemiluminescence. Quantification of the relative amounts of bands C and GAPDH was performed by using NIH ImageJ analysis of scanned films [1]. |
| 激酶實(shí)驗(yàn) | In one set of assays, R1070W-?F508-CFTR-HRP (R1070W-HRP)–expressing CFBE41o? cells were incubated with 100 μl medium containing 25 μM test compounds and 0.5 μg/ml doxycycline for 24 hours at 37°C. In a second set of assays, ?F508-CFTR-HRP (?F508-HRP)–expressing CFBE41o? cells were incubated with 100 μl medium containing 25 μM test compounds, 2 μM VX-809, and 0.5 μg/ml doxycycline for 24 hours at 37°C. All compound plates contained negative controls (DMSO vehicle) and positive controls [2 μM VX-809]. In both assays, the cells were washed four times with PBS, and HRP activity was assayed by the addition of 50 μl/well of HRP substrate. After shaking for 5 minutes, chemiluminescence was measured using a Tecan Infinite M1000 plate reader (Tecan Groups Ltd, Mannedorf, Switzerland) equipped with an automated stacker (integration time, 100 milliseconds). Z′ is defined as = 1 ? [(3 × standard deviation of maximum signal control + 3 × standard deviation of minimum signal control)/absolute (mean of maximum signal control ? mean of minimum signal control)] [2]. |
| 體外活性 | In cultured human bronchial epithelial cells isolated from patients with CF homozygous for F508del, Lumacaftor (VX-809) improved F508del-CFTR processing in the endoplasmic reticulum and enhanced chloride secretion to approximately 14% of non-CF human bronchial epithelial cells (EC50: 81 nM), a level associated with mild CF in patients with less disruptive CFTR mutations [1]. VX-809 produced a concentration-dependent increase in the HRP luminescence signal after incubation with cells at 37°C or 27°C in both cell lines, with a similar EC50 value of approximately 0.3 μM [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 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 6 mg/mL (13.26 mM) DMSO : 50 mg/mL (110.52 mM) |
| 關(guān)鍵字 | VX 809 | VX809 | CFTR | Cystic fibrosis transmembrane conductance regulator | VRT826809 | Inhibitor | VRT-826809 | Lumacaftor | inhibit | Autophagy |
| 相關(guān)產(chǎn)品 | Stavudine | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | EMA 上市藥物庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | FDA 上市藥物庫(kù) | 抗癌上市藥物庫(kù) | 已知活性化合物庫(kù) | 離子通道庫(kù) | 抗癌藥物庫(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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