價格 | ¥262 | ¥369 | ¥578 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-12 |
中文名稱:化合物 JAK3-IN-6 | 英文名稱:JAK3-IN-6 |
CAS:1443235-95-7 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.94% | 產(chǎn)品類別: 抑制劑 |
貨號: T5492 |
名稱 | JAK3-IN-6 |
描述 | JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM |
動物實驗 | Female Lewis rats were purchased and housed . 48 rats were divided into six groups (n=8/group). Group 1 were drug-na?ve i.e. no compounds were administered throughout the study. On the afternoon of Day 1 (4pm), ABT or vehicle (1 ml/kg p.o.) was administered to Groups 2-5. Days 2-11 (8 am), each animal in Groups 2-5 were administered ABT 10 mpk qd (1 ml/kg p.o.), immediately followed by either vehicle or compound at 5ml/kg p.o. Group 6 animals received vehicle only (5 ml/kg p.o.). Days 2-11 (4 pm) Groups 2-5 were administered vehicle or compound at 5 ml/kg p.o. Animals were monitored and weighed throughout the study. On Day 10, under isoflurane anesthesia, 3 animals from Groups 2-6 were bled via the jugular vein for PK analysis at 4 and 8 h post-8 am dose. On Day 11, blood samples were collected, as described above, at 0 (16 h post-Day 10 pm dose) and 2 h post-am dose for PK, hematology, and clinical chemistry analysis. All remaining animals were euthanized at 2 hrs post-dosing on Day 11 and blood samples were collected for PK, hematology, and clinical chemistry analysis. Data were analyzed using Graphpad prism software. Statistical analyses were performed using a one-way ANOVA with Dunnett s post-hoc test for group comparisons to ABT + vehicle treatment. |
體外活性 | 一種強效的JAK3抑制劑(0.15 nM)在酶類實驗中對JAK3的選擇性是對JAK1的4300倍,而在細(xì)胞報告實驗中對IL-2相比IL-6的選擇性是67倍,對IL-2相比EPO或GMCSF的選擇性是140倍,在人類PBMC實驗中對IL-7相比IL-6或GMCSF的選擇性是大于35倍。在體內(nèi),選擇性抑制JAK3足以阻斷炎癥在類風(fēng)濕關(guān)節(jié)炎大鼠模型中的發(fā)展,并且不影響造血。 |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 40 mg/mL (114.17 mM), Sonication is recommended. |
關(guān)鍵字 | inhibit | JAK3 IN 6 | JAK | Inhibitor | JAK3IN6 | JAK3-IN-6 | JAK-3-IN-6 | Janus kinase |
相關(guān)產(chǎn)品 | JAK-IN-10 | Tofacitinib Citrate | Deucravacitinib | RO8191 | Ruxolitinib | KW-2449 | TAK-901 | CEP-33779 | Baricitinib | Fedratinib | Ruxolitinib phosphate | Delgocitinib |
相關(guān)庫 | 抑制劑庫 | 血管生成庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 高選擇性抑制劑庫 | 抗衰老化合物庫 | NO PAINS 化合物庫 | 表觀遺傳庫 | 表型篩選靶點鑒定庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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