Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Delgocitinib (Corectim(Delgocitinib)) 是一种有效的、有特异性的 JAK 抑制剂,对 JAK1, JAK2, JAK3 和 Tyk2 具有抑制作用,其 IC50 值分别为 2.8,2.6,13 和 58 nM。Delgocitinib 通过JAK-依赖性细胞因子参与多种炎症和自身免疫性疾病,可广泛用于治疗各种炎症性疾病,是全球首款治疗特应性皮炎的JAK 局部外用化合物。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,380 | 现货 | ||
5 mg | ¥ 3,460 | 现货 | ||
10 mg | ¥ 4,920 | 现货 | ||
25 mg | ¥ 7,860 | 现货 | ||
50 mg | ¥ 10,500 | 现货 | ||
100 mg | ¥ 14,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,530 | 现货 |
产品描述 | Delgocitinib (Corectim(Delgocitinib)) is a potent and specific JAK inhibitor with an IC50 value of 2.8, 2.6, 13 and 58 nM against JAK1, JAK2, JAK3 and Tyk2. Delgocitinib is involved in a variety of inflammatory and autoimmune diseases through JAK-dependent cytokines and can be widely used in the treatment of various inflammatory diseases. Delgocitinib is the world's first JAK topical compound for the treatment of atopic dermatitis. |
靶点活性 | JAK2:2.6 nM, JAK1:2.8 nM, TYK2:58 nM, JAK3:13 nM |
体外活性 | Delgocitinib inhibits the phosphorylation of Stat proteins induced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α (IC50: 40±9, 33±14, 84±11, 304±22 and 18±3 nM, respectively), in these cell-based cytokine signaling assays and it also inhibits IL-2-induced proliferation of T cells in a concentration-dependent manner (IC50: 8.9±3.6 nM). Its potency is similar to that of tofacitinib (IC50:16 nM). Delgocitinib effectively inhibits all of the JAK subtypes ( IC50: 2.8±0.6, 2.6±0.2, 13±0 and 58±9 nM for JAK1, JAK2, JAK3 and Tyk2, respectively), in the enzymatic assays. Lineweaver-Burk plots display that the inhibition mode of Delgocitinib toward all JAKs is competitive with ATP (Ki: 2.1±0.3, 1.7±0.0, 5.5±0.3 and 14±1 nM for JAK1, JAK2, JAK3 and Tyk2, respectively) [1]. |
体内活性 | Delgocitinib inhibits radiographic and histological changes of bone destruction and cartilage destruction. Delgocitinib induces the IFN-γ production, however, the potency of the 1-h prior administration(ED50: 0.24 mg/kg) is higher than that of the 6-h prior administration (ED50: 1.3 mg/kg). In the administration from day 1, Delgocitinib prevents the development of hind paw swelling and histological changes of inflammatory cell infiltration and synovial cell hyperplasia. In the administration from day 15, Delgocitinib decreases the paw swelling in a dose-dependent manner. Delgocitinib ameliorates the inflammatory cell infiltration, synovial cell hyperplasia, and cartilage/bone destructions in the histological and radiographic examinations at the end of the study[1]. |
别名 | JTE-052, 迪高替尼, Corectim(Delgocitinib) |
分子量 | 310.35 |
分子式 | C16H18N6O |
CAS No. | 1263774-59-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (161.11 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2222 mL | 16.1108 mL | 32.2217 mL | 80.5542 mL |
5 mM | 0.6444 mL | 3.2222 mL | 6.4443 mL | 16.1108 mL | |
10 mM | 0.3222 mL | 1.6111 mL | 3.2222 mL | 8.0554 mL | |
20 mM | 0.1611 mL | 0.8055 mL | 1.6111 mL | 4.0277 mL | |
50 mM | 0.0644 mL | 0.3222 mL | 0.6444 mL | 1.6111 mL | |
100 mM | 0.0322 mL | 0.1611 mL | 0.3222 mL | 0.8055 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Delgocitinib 1263774-59-9 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK Inhibitor Corectim Janus kinase inhibit JTE 052 JTE-052 迪高替尼 Corectim(Delgocitinib) JTE052 inhibitor