Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Voclosporin (ISAtx-247) 是一种新型且可口服钙调磷酸酶(CN; PP2B)抑制剂和免疫抑制剂,可用于治疗狼疮性肾炎。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,390 | 现货 | ||
5 mg | ¥ 3,730 | 现货 | ||
10 mg | ¥ 5,990 | 现货 | ||
25 mg | ¥ 8,890 | 现货 | ||
50 mg | ¥ 11,900 | 现货 | ||
100 mg | ¥ 15,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 7,830 | 现货 |
产品描述 | Voclosporin (ISAtx-247) is a novel and orally available calcium-modulated phosphatase (CN; PP2B) inhibitor and immunosuppressant for the treatment of lupus nephritis. |
体外活性 | Voclosporin (ISATX247) is a calcineurin inhibitor that has shown more potency than Cyclosporine in vitro.[2] |
体内活性 | Voclosporin (23.7 mg or 39.5 mg, each twice daily; 265 subjects; 48 weeks) versus placebo in combination with mycophenolate mofetil (2 g/d) and rapidly tapered low-dose oral corticosteroids for induction of remission in LN. CRR at week 24 was achieved by 29 (32.6%) subjects in the low-dose voclosporin group, 24 (27.3%) subjects in the high-dose voclosporin group, and 17 (19.3%) subjects in the placebo group (OR=2.03 for low-dose voclosporin versus placebo). The significantly greater CRR rate in the low-dose voclosporin group persisted at 48 weeks, and CRRs were also significantly more common in the high-dose voclosporin group compared to placebo at 48 weeks. There were more serious adverse events in both voclosporin groups, and more deaths in the low-dose group compared to placebo and high-dose voclosporin groups (11.2%, 1.1%, and 2.3%, respectively). These results suggest that the addition of low-dose voclosporin to mycophenolate mofetil and corticosteroids for induction therapy of active LN results in a superior renal response compared to mycophenolate mofetil and corticosteroids alone, but higher rates of adverse events including death were observed.[3] |
别名 | ISAtx-247 |
分子量 | 1214.62 |
分子式 | C63H111N11O12 |
CAS No. | 515814-01-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45.0 mg/mL (37.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 0.8233 mL | 4.1165 mL | 8.233 mL | 20.5826 mL |
5 mM | 0.1647 mL | 0.8233 mL | 1.6466 mL | 4.1165 mL | |
10 mM | 0.0823 mL | 0.4117 mL | 0.8233 mL | 2.0583 mL | |
20 mM | 0.0412 mL | 0.2058 mL | 0.4117 mL | 1.0291 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。
Voclosporin 515814-01-4 Metabolism Phosphatase ISAtx-247 Inhibitor inhibitor inhibit