Elastatinal
(Synonyms: (2S)-2-[(4S)-2-氨基-1,4,5,6-四羟基4-嘧啶基]-N-[[[(1S)-1-羰基-3-甲基丁基]氨基]羰基]甘氨酰-N1-[(1S)-1-甲基-2-氧乙基-L-谷氨酸甲酰胺) 目录号 : GC18191A potent inhibitor of pancreatic elastase
Cas No.:51798-45-9
Sample solution is provided at 25 µL, 10mM.
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Elastatinal is a potent inhibitor of pancreatic elastase (Ki = 240 nM) that is produced by various species of Actinomycetes. [1] It more strongly inhibits pancreatic elastase versus the leukocyte-derived enzyme. [2] [3] Elastatinal reduces electrophoretic mobilities of 2A proteinases from poliovirus and human rhinovirus 14 in a dose-dependent manner, indicating substrate recognition by 2A proteinases is similar to that of pancreatic elastases.[4] It can also inhibit elastase-like protease collagenolytic protease from C. maenas digestive glands.[5]
Reference:
[1]. Umezawa, H. Structures and activities of protease inhibitors of microbial origin. Methods Enzymol. 45, 678-695 (1976).
[2]. Feinstein, G., Malemud, C.J., and Janoff, A. The inhibition of human leucocyte elastase and chymotrypsin-like protease by elastatinal and chymostatin. Biochim Biophys. Acta. 429(3), 925-932 (1976).
[3]. Okumura, Y., Ogawa, K., and Uchiya, K. Characterization and primary structure of elastase inhibitor, AFLEI, from Aspergillus flavus. Nishon Ishinkin Gakkai Zasshi 48(1), 13-18 (2007).
[4]. Molla, A., Hellen, C.U.T., and Wimmer, E. Inhibition of proteolytic activity of poliovirus and rhinovirus 2A proteinases by elastase-specific inhibitors. J. Virol. 67(8), 4688-4695 (1993).
[5]. Roy, P., Colas, B., and Durand, P. Purification, kinetical and molecular characterizations of a serine collagenolytic protease from greenshore crag (Carcinus maenas) digestive gland. Comp. Biochem. Physiol. Biochem. Mol. Biol. 115(1), 87-95 (1996).
| Cas No. | 51798-45-9 | SDF | |
| 别名 | (2S)-2-[(4S)-2-氨基-1,4,5,6-四羟基4-嘧啶基]-N-[[[(1S)-1-羰基-3-甲基丁基]氨基]羰基]甘氨酰-N1-[(1S)-1-甲基-2-氧乙基-L-谷氨酸甲酰胺 | ||
| 化学名 | (2S)-2-[(4S)-2-amino-3,4,5,6-tetrahydro-4-pyrimidinyl]-N-[[[(1S)-1-carboxy-3-methylbutyl]amino]carbonyl]glycyl-N1-[(1S)-1-methyl-2-oxyethyl]-L-glutamamide | ||
| Canonical SMILES | NC1=NCC[C@]([C@H](NC(N[C@H](C(O)=O)CC(C)C)=O)C(N[C@H](C(N[C@@H](C)C=O)=O)CCC(N)=O)=O)([H])N1 | ||
| 分子式 | C21H36N8O7 | 分子量 | 512.6 |
| 溶解度 | 20mg/mL in DMSO, 33mg/mL in DMF | 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 | 1.9508 mL | 9.7542 mL | 19.5084 mL |
| 5 mM | 0.3902 mL | 1.9508 mL | 3.9017 mL |
| 10 mM | 0.1951 mL | 0.9754 mL | 1.9508 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: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet