GSK-2793660
目录号 : GC62634
GSK-2793660（游离碱）是一种口服的、不可逆的组织蛋白酶 C (CTSC) 抑制剂。
Cas No.:1613458-70-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GSK-2793660 is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis[1][2].
GSK-2793660 is a cathepsin C (also known as dipeptidyl peptidase I enzyme) inhibitor for the reaearch of cystic fibrosis, non-cystic fibrosis bronchiectasis, anti-neutrophil cytoplasmic autoantibody (ANCA)-associated vasculitis and bronchiectasis[1].
[1]. Szcze?niak P, et al. The Synthesis of α,α-Disubstituted α-Amino Acids via Ichikawa Rearrangement. J Org Chem. 2016 Feb 5;81(3):1057-74.
[2]. Miller BE, et al. Epithelial desquamation observed in a phase I study of an oral cathepsin C inhibitor (GSK2793660). Br J Clin Pharmacol. 2017 Dec;83(12):2813-2820.
| Cas No. | 1613458-70-0 | SDF | |
| 分子式 | C20H27N3O3 | 分子量 | 357.45 |
| 溶解度 | DMSO : 100 mg/mL (253.87 mM; Need ultrasonic) | 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 | 2.7976 mL | 13.988 mL | 27.9759 mL |
| 5 mM | 0.5595 mL | 2.7976 mL | 5.5952 mL |
| 10 mM | 0.2798 mL | 1.3988 mL | 2.7976 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。
The Synthesis of α,α-Disubstituted α-Amino Acids via Ichikawa Rearrangement
J Org Chem 2016 Feb 5;81(3):1057-74.PMID:26726732DOI:10.1021/acs.joc.5b02628.
An approach to α,α-disubstituted α-amino acids is reported. The key step is allyl cyanate-to-isocyanate rearrangement. As demonstrated, the resultant allyl isocyanates can be directly trapped with various nucleophiles, for instance, alcohols, amines, and organometallic reagents, to provide a broad range of N-functionalized allylamines. The developed method has been successfully applied in the synthesis of two bioactive peptides: 2-aminoadamantane-2-carboxylic acid derived P2X7-evoked glutamate release inhibitor and 4-amino-tetrahydropyranyl-4-carboxylic acid derived dipeptide GSK-2793660, which is currently in clinical trials as cathepsin C inhibitor for the treatment of cystic fibrosis, noncystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis.