Powder: -20°C for 3 years | In solvent: -80°C for 1 year
P505-15 Acetate 是脾脏酪氨酸激酶的选择性抑制剂,通过抑制白细胞免疫功能和炎症起作用,导致关节炎评分降低和组织学损伤减轻。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,290 | 现货 | ||
5 mg | ¥ 2,990 | 现货 | ||
10 mg | ¥ 4,390 | 现货 | ||
25 mg | ¥ 6,910 | 现货 | ||
50 mg | ¥ 9,480 | 现货 | ||
100 mg | ¥ 12,800 | 现货 | ||
500 mg | ¥ 25,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,290 | 现货 |
产品描述 | P505-15 Acetate is a selective inhibitor of spleen tyrosine kinase that acts by suppressing leukocyte immune function and inflammation and leading to a reduction in arthritis score and attenuated histological damage. |
靶点活性 | Syk kinase:1-2 nM |
体外活性 | In human whole blood, P505-15 potently inhibited B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC50 0.15 μM) [1]. P505-15 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL [2]. PRT318 and P505-15 effectively antagonize CLL cell survival after BCR triggering and in nurse-like cell-co-cultures. Moreover, they inhibit BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT318 and P505-15 furthermore inhibit Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering [3]. |
体内活性 | Similar levels of ex vivo inhibition were measured after dosing in mice (Syk signaling IC50 0.32 μM). Oral administration of P505-15 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis [1]. Oral dosing in mice prevented BCR-mediated splenomegaly and significantly inhibited NHL tumor growth in a xenograft model. In addition, combination treatment of primary CLL cells with P505-15 plus fludarabine produced synergistic enhancement of activity at nanomolar concentrations [2]. |
别名 | PRT 062607 Acetate, P505 15 Acetate, PRT-062607 Acetate, PRT062607 Acetate, P50515 Acetate |
分子量 | 453.5 |
分子式 | C21H27N9O3 |
CAS No. | 1370261-98-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (22.05 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2051 mL | 11.0254 mL | 22.0507 mL | 55.1268 mL |
5 mM | 0.441 mL | 2.2051 mL | 4.4101 mL | 11.0254 mL | |
10 mM | 0.2205 mL | 1.1025 mL | 2.2051 mL | 5.5127 mL | |
20 mM | 0.1103 mL | 0.5513 mL | 1.1025 mL | 2.7563 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。
P505-15 Acetate 1370261-98-5 Proteases/Proteasome Tyrosinase PRT 062607 Acetate P 50515 Acetate P-50515 Acetate P505 15 Acetate PRT-062607 Acetate PRT062607 Acetate P50515 Acetate Inhibitor inhibitor inhibit