| CAS NO: | 100938-10-1 |
| 包装 | 价格(元) |
| 500ug | 电议 |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 511.01 |
| Cas No. | 100938-10-1 |
| Formula | C21H39ClN4O8 |
| Solubility | ≤1mg/ml in ethanol;2mg/ml in DMSO;10mg/ml in dimethyl formamide |
| Chemical Name | (S)-2-((S)-2-((S)-2-((2S,3R)-3-amino-2-hydroxy-5-methylhexanamido)-3-methylbutanamido)-3-methylbutanamido)succinic acid hydrochloride |
| Canonical SMILES | CC(C)[C@H](NC([C@@H](NC([C@@H](O)[C@H](N)CC(C)C)=O)C(C)C)=O)C(N[C@@H](CC(O)=O)C(O)=O)=O.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Amastatin (hydrochloride) is a competitive inhibitor of various aminopeptidases with slow but strong binding (Ki = 0.26, 30 and 52 nM forAeromonas aminopeptidase, cytosolic leucine aminopeptidase and microsomal aminopeptidase) [1].
Aminopeptidases, found in many subcellular organelles, in cytosol, and as membrane components, are enzymes that catalyze the cleavage of amino acids from the amino of proteins or peptides. Aminopeptidases play important roles in various essential cellular functions [1].
Amastatin (10 μg/ml ~ 1 mg/ml) exhibited dose-dependent inhibitory profiles onE. cuniczcli replicationin vitro [2]. In addition, in spleen lymphocyte cultures with macrophages, Amastatin stimulated [3H]thymidine incorporation into lymphocytes/macrophages, with the optimal stimulatory concentration around 0.1 μg/ml [3].
In anesthesized rats, infusion of amastatin (16 nmol/min i.v.) only slightly increased the potency of angiotensin I and AII, whilst significantly increased the potency of AIII and des(Asp1)angiotensin I. Furthermore, amastatin specifically inhibited plasma aminopeptidase M and aminopeptidase A activities by 81% and 10%, respectively [4].
References:
[1]. Wilkes S H, Prescott J M. The slow, tight binding of bestatin and amastatin to aminopeptidases. Journal of Biological Chemistry, 1985, 260(24): 13154-13162.
[2]. Millership J J, Didier E S, Okhuysen P C, et al. In vitro and in vivo evaluation of aminopeptidase inhibitors as antimicrosporidial therapies. Journal of Eukaryotic Microbiology, 2001, Suppl: 95S-98S.
[3]. Weissmann N, Leyhausen G, Maidhof A, et al. Mitogenic potentials of bestatin, amastatin, arphamenines A and B, FK-156 and FK-565 on spleen lymphocytes. The Journal of Antibiotics, 1985, 38(6): 772-778.
[4]. Ahmad S, Ward P E. Role of aminopeptidase activity in the regulation of the pressor activity of circulating angiotensins. Journal of Pharmacology and Experimental Therapeutics, 1990, 252(2): 643-650.
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