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Voclosporin

Voclosporin

产品编号 T17235   CAS 515814-01-4
别名: ISAtx-247

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。

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Voclosporin Chemical Structure
Voclosporin, CAS 515814-01-4
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Voclosporin (T17235)
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纯度: 99.85%
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存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 45.0 mg/mL (37.1 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Abel MD, et al. ISATX247: a novel calcineurin inhibitor. J Heart Lung Transplant. 2001 Feb;20(2):161. 2. Stalder M, et al. In vivo evaluation of the novel calcineurin inhibitor ISATX247 in non-human primates. J Heart Lung Transplant. 2003 Dec;22(12):1343-52. 3. Rovin BH, et al. A randomized, controlled double-blind study comparing the efficacy and safety of dose-ranging voclosporin with placebo in achieving remission in patients with active lupus nephritis. Kidney Int. 2019;95(1):219-231. 4. Arriens C, et al. Update on the Efficacy and Safety Profile of Voclosporin: An Integrated Analysis of Clinical Trials in Lupus Nephritis. Arthritis Care Res (Hoboken). 2023;75(7):1399-1408. 5. Cunningham MA, et al. LX211 (voclosporin) suppresses experimental uveitis and inhibits human T cells. Invest Ophthalmol Vis Sci. 2009;50(1):249-255.
Atraric acid h-NTPDase-IN-1 SMAP-2 Raphin1 3-Acetoxy-11-ursen-28,13-olide BCI Sephin1 DJ001

相关化合物库

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上市药物库 FDA上市及药典收录分子库

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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。

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Keywords

Voclosporin 515814-01-4 Metabolism Phosphatase ISAtx-247 Inhibitor inhibitor inhibit

 

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