Pepstatin A (Synonyms: NSC 272671, Pepsin Inhibitor S 735A) |
| Katalog-Nr.GC11974 |
Pepstatin A is an orally active inhibitor of aspartic proteases, which is produced by actinomycetes.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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. |
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Reaction Conditions |
0-120 µM |
|
Applications |
Pepstatin A suppressed the formation of TRAP-positive multinuclear cells in a dose-dependent manner. |
| Animal experiment [2]: | |
|
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 | |
| Überlieferungen | NSC 272671, Pepsin Inhibitor S 735A | ||
| Chemical Name | 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 | ||
| Formula | C34H63N5O9 | M.Wt | 685.9 |
| Löslichkeit | ≥ 34.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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