GSK256066 NEW
| Price | $33 | $47 | $76 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-16 |
Product Details
| Product Name: GSK256066 | CAS No.: 801312-28-7 |
| Purity: 99.66% | Supply Ability: 10g |
| Release date: 2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | GSK256066 |
| 描述 | GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380, 000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2. |
| 體外活性 | GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 x 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 x 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity. [1] |
| 體內(nèi)活性 | GSK256066 inhibits the LPS-induced pulmonary neutrophilia with an ED50 of 1.1 μg/kg, achieving maximal inhibition of 72% at 30 μg/kg when given in the aqueous suspension. GSK256066 inhibits the LPS-induced pulmonary neutrophilia with ED50 of 2.9 μg/kg, achieving maximal inhibition of 62% when given in the dry powder formulation. GSK256066 shows a moderate plasma clearance of 39 ml/min/kg, a moderate volume of distribution of 0.8 L/kg, and a relatively short half-life of 1.1 hour in the male CD rat. [1] GSK256066 sustains at a high lung concentration of 2.6 μg/g after intra-tracheal administration as an aqueous suspension at a dose of 30 μg/kg in rats. [2] GSK256066 (10 μg/kg) is administered intratracheally at different times (2, 6, 12, 18, 24, and 36 hours) before LPS administration, inhibiting LPS-Induced Pulmonary Neutrophilia in rat lipopolysaccharide (LPS)-induced models of acute pulmonary inflammation. GSK256066 (0.3–100 μg/kg) inhibits LPS-induced increases in exhaled nitric oxide with ED50 of 35 μg/kg in rat. GSK256066 (10 μg/kg) is administered half a hour before OVA administration in rat, inhibiting OVA-induced pulmonary eosinophilia with ED50 of 0.4 μg/kg. GSK256066 administered intratracheally as a dry powder blended in respiratory-grade lactose at doses of 3 to 100 μg/kg 2 hours before inhaled LPS challenge in ferrets, inhibiting LPS-induced pulmonary neutrophilia with ED50 of 18 μg/kg without inducing emetic episodes. [3] |
| 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 : 10 mg/mL (19.28 mM) |
| 關(guān)鍵字 | Phosphodiesterase (PDE) | PDE | obstructive | disease | chronic | high-affinity | inhibit | phosphodiesterase | PDE4B | Inhibitor | GSK 256066 | pulmonary | GSK256066 | GSK-256066 |
| 相關(guān)產(chǎn)品 | Theophylline monohydrate | Diphylline | Acefylline | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline |
| 相關(guān)庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 抗阿爾茨海默癥化合物庫(kù) | ReFRAME 相關(guān)化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 臨床期小分子藥物庫(kù) | 已知活性化合物庫(kù) | 抗代謝疾病化合物庫(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
- Address: 36?Washington?Street, Wellesley?Hills
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