Voclosporin (ISAtx-247)
(Synonyms: ISAtx-247) 目录号 : GC31769
Voclosporin (ISAtx-247) (ISAtx-247) 是一种钙调神经磷酸酶 (PP2B) (CN) 抑制剂。
Cas No.:515814-01-4
Sample solution is provided at 25 µL, 10mM.
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Voclosporin is a calcineurin (CN) inhibitor.
This novel semi-synthetic calcineurin (CN) inhibitor is designated Voclosporin (ISATX247). The efficacy of Voclosporin as an immunosuppressive agent is examined using an in vitro calcineurin assay[1]. Voclosporin (ISATX247) is a calcineurin inhibitor that has shown more potency than Cyclosporine in vitro[2].
All animals tolerate Voclosporin (ISATX247) and Cyclosporine A (CsA) very well. There are no severe adverse effects associated with either drug. In the Voclosporin group, all animals except 1 have diarrhea of different durations during the study (mean 2.3 days, range 2 to 7 days). This differs from the CsA and the control groups, where no animals have diarrhea. Mean weight loss at the end of the study is slightly higher in the Voclosporin group than in the CsA and control groups (3.4% vs 2.0% and 1.0%, respectively)[2].
[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.
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Animal experiment: |
Monkey[2] Wild-caught, male cynomolgus monkeys, weighing between 5 and 8 kg, are used. Four groups of animals are treated twice daily at 8:00 AM and 6:00 PM for 7 days with the following doses: Group I (n=6), Voclosporin 25 mg/kg; Group II (n=6), Voclosporin 50 mg/kg; Group III (n=5), CsA 25 mg/kg; and Group IV (n=4), vehicle (no drug) 1 mL/kg. Levels of Cyclosporine and Voclosporin in whole blood are measured by liquid chromatography/mass spectrometry[2]. |
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References: [1]. Abel MD, et al. ISATX247: a novel calcineurin inhibitor. J Heart Lung Transplant. 2001 Feb;20(2):161. |
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| Cas No. | 515814-01-4 | SDF | |
| 别名 | ISAtx-247 | ||
| Canonical SMILES | C=C/C=C/C[C@@H](C)[C@H]([C@]1([H])N(C([C@](N(C([C@@H](N(C([C@](N(C([C@H](NC([C@@H](NC([C@H](CC(C)C)N(C)C([C@@](C(C)C)([H])NC([C@H](CC(C)C)N(C)C(CN(C)C([C@H](CC)NC1=O)=O)=O)=O)=O)=O)C)=O)C)=O)C)([H])CC(C)C)=O)C)CC(C)C)=O)C)([H])C(C)C)=O)C)O | ||
| 分子式 | C63H111N11O12 | 分子量 | 1214.62 |
| 溶解度 | DMSO : ≥ 50 mg/mL (41.17 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.8233 mL | 4.1165 mL | 8.233 mL |
| 5 mM | 0.1647 mL | 0.8233 mL | 1.6466 mL |
| 10 mM | 0.0823 mL | 0.4117 mL | 0.8233 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet