Pepstatin A
(Synonyms: 抑肽素; Pepstatin A) 目录号 : GC11974
胃抑素Pepstatin A是由放线菌类产生的一种特异性的、具有口服活性的天冬氨酸蛋白酶 (aspartic proteases) 抑制剂,能够抑制 hemoglobin-pepsin、hemoglobin-proctase、casein-pepsin、casein-proctase、casein-acid protease 和 hemoglobin-acid protease 的活性,IC50 值分别为 4.5 nM、6.2 nM、150 nM、290 nM、520 nM 和 260 nM；Pepstatin A可抑制 HIV protease 的活性.Pepstatin A (0-120 µM) 抑制了受体活化因子NF-κB配体(RANKL)-诱导的破骨细胞分化。
Cas No.:26305-03-3
Sample solution is provided at 25 µL, 10mM.
Pepstatin A is an orally active inhibitor of aspartic proteases, which is produced by actinomycetes. It exhibits inhibitory activity with IC50 values of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM, and 260 nM against hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease, and hemoglobin-acid protease, respectively. Additionally, pepstatin has been found to inhibit HIV protease [1-3].
Pepstatin A(0-120 µM) suppressed receptor activator of NF-κB ligand (RANKL)-induced osteoclast differentiation[4]. Pepstatin A(0.1-0.3 µM) caused a reproducible, concentration-related increase in the extracellular acidification rate in two microglial cell lines, Ra2 and 6-3[5]. Pepstatin A significantly hindered influenza virus replication, probably by modulating host cell autophagic/apoptotic responses[6].
Pepstatin (0.5-50 mg/kg; p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats[1].
References:
[1]. Yoshida H, Okamoto K, et,al. Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. J Biochem. 2006 Mar;139(3):583-90. doi: 10.1093/jb/mvj066. PMID: 16567424.
[2]. Seelmeier S, Schmidt H, et,al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6. doi: 10.1073/pnas.85.18.6612. PMID: 3045820; PMCID: PMC282027.
[3]. Seelmeier S, Schmidt H, et,al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6. doi: 10.1073/pnas.85.18.6612. PMID: 3045820; PMCID: PMC282027.
[4]. Yoshida H, Okamoto K, et,al.Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. J Biochem. 2006 Mar;139(3):583-90. doi: 10.1093/jb/mvj066. PMID: 16567424.
[5]. Okada M, Irie S, S et,al. Pepstatin A induces extracellular acidification distinct from aspartic protease inhibition in microglial cell lines. Glia. 2003 Aug;43(2):167-74. doi: 10.1002/glia.10237. PMID: 12838508.
[6]. Matarrese P, Nencioni L, et,al. Pepstatin A alters host cell autophagic machinery and leads to a decrease in influenza A virus production. J Cell Physiol. 2011 Dec;226(12):3368-77. doi: 10.1002/jcp.22696. PMID: 21344392.
胃抑素Pepstatin A是由放线菌类产生的一种特异性的、具有口服活性的天冬氨酸蛋白酶 (aspartic proteases) 抑制剂,能够抑制 hemoglobin-pepsin、hemoglobin-proctase、casein-pepsin、casein-proctase、casein-acid protease 和 hemoglobin-acid protease 的活性,IC50 值分别为 4.5 nM、6.2 nM、150 nM、290 nM、520 nM 和 260 nM；Pepstatin A可抑制 HIV protease 的活性[1-3].
Pepstatin A (0-120 µM) 抑制了受体活化因子NF-κB配体(RANKL)-诱导的破骨细胞分化[4]。Pepstatin A (0.1-0.3 µM) 可以在两个微胶质细胞系Ra2和6-3中引起浓度相关的可重复的细胞外酸化率增加[5]。Pepstatin A 显著阻碍了流感病毒的复制,可能是通过调节宿主细胞自噬/凋亡反应发挥作用[6]。
Pepstatin A (0.5-50 mg/kg; p.o.)对结扎的谢氏大鼠幽门溃疡有抑制作用[1]。
| Cell experiment [1]: | |
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Cell lines |
Osteoclasts |
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Preparation Method |
Pepstatin A was added at 15-120 µM to the growth medium. |
|
Reaction Conditions |
0-120 µM |
|
Applications |
Pepstatin A suppressed the formation of TRAP-positive multinuclear cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Ligated Shay rats |
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Dosage form |
0.5-50 mg/kg, p.o. |
|
Applications |
After using Pepstatin A, free sialic acid and bound sialic acid were decreased in the gastric juice of the Shay rats. |
|
References: [1]. Yoshida H, Okamoto K, et,al. Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. J Biochem. 2006 Mar;139(3):583-90. doi: 10.1093/jb/mvj066. PMID: 16567424. |
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| Cas No. | 26305-03-3 | SDF | |
| 别名 | 抑肽素; Pepstatin A | ||
| 化学名 | 3-hydroxy-4-[2-[[3-hydroxy-6-methyl-4-[[3-methyl-2-[[3-methyl-2-(3-methylbutanoylamino)butanoyl]amino]butanoyl]amino]heptanoyl]amino]propanoylamino]-6-methylheptanoic acid | ||
| Canonical SMILES | CC(C)CC(C(CC(=O)O)O)NC(=O)C(C)NC(=O)CC(C(CC(C)C)NC(=O)C(C(C)C)NC(=O)C(C(C)C)NC(=O)CC(C)C)O | ||
| 分子式 | C34H63N5O9 | 分子量 | 685.9 |
| 溶解度 | ≥ 34.3mg/mL in DMSO | 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 | 1.4579 mL | 7.2897 mL | 14.5794 mL |
| 5 mM | 0.2916 mL | 1.4579 mL | 2.9159 mL |
| 10 mM | 0.1458 mL | 0.729 mL | 1.4579 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
