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Apstatin (CAS 160470-73-5)

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Alternate Names:
Aminopeptidase P Inhibitor; N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]-L-prolyl-L-prolyl-L-alaninamide
Application:
Apstatin is a selective inhibitor of Aminopeptidase P (APP)
CAS Number:
160470-73-5
Purity:
≥95%
Molecular Weight:
459.54
Molecular Formula:
C23H33N5O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Apstatin is a selective inhibitor of aminopeptidase P (APP), with a Ki of 2.6 muM in rat lung membrane-bound APP. Apstatin is shown to increase Bradykinin-promoted cardioprotection in rats with artificially introduced myocardial infarctions by inhibiting the Bradykinin degradation action of APP. When combined with the angiotensin-converting enzyme inhibitors enalapril (sc-205664), lisinopril (sc-205378), or ramipril (sc-205833), decrease of myocardial infarction size was enhanced.


Apstatin (CAS 160470-73-5) References

  1. Cardioprotective effects of the aminopeptidase P inhibitor apstatin: studies on ischemia/reperfusion injury in the isolated rat heart.  |  Erşahin, C., et al. 1999. J Cardiovasc Pharmacol. 34: 604-11. PMID: 10511138
  2. Effects of the aminopeptidase P inhibitor apstatin on bradykinin-induced inositol 1,4,5-triphosphate in neonatal rat cardiomyocytes.  |  Kudoh, A., et al. 2001. J Cardiovasc Pharmacol. 37: 495-501. PMID: 11336100
  3. Apstatin, a selective inhibitor of aminopeptidase P, reduces myocardial infarct size by a kinin-dependent pathway.  |  Wolfrum, S., et al. 2001. Br J Pharmacol. 134: 370-4. PMID: 11564655
  4. Infarct size limiting effect of apstatin alone and in combination with enalapril, lisinopril and ramipril in rats with experimental myocardial infarction.  |  Veeravalli, KK., et al. 2003. Pharmacol Res. 48: 557-63. PMID: 14527819
  5. Structure of Escherichia coli aminopeptidase P in complex with the inhibitor apstatin.  |  Graham, SC., et al. 2004. Acta Crystallogr D Biol Crystallogr. 60: 1770-9. PMID: 15388923
  6. Crystal structure of X-prolyl aminopeptidase from Caenorhabditis elegans: A cytosolic enzyme with a di-nuclear active site.  |  Iyer, S., et al. 2015. FEBS Open Bio. 5: 292-302. PMID: 25905034
  7. Structure of the human aminopeptidase XPNPEP3 and comparison of its in vitro activity with Icp55 orthologs: Insights into diverse cellular processes.  |  Singh, R., et al. 2017. J Biol Chem. 292: 10035-10047. PMID: 28476889
  8. Angiotensin-Converting Enzyme Inhibitor Protects Against Cisplatin Nephrotoxicity by Modulating Kinin B1 Receptor Expression and Aminopeptidase P Activity in Mice.  |  Estrela, GR., et al. 2020. Front Mol Biosci. 7: 96. PMID: 32528973
  9. Potentiation by aminopeptidase P of blood pressure response to bradykinin.  |  Kitamura, S., et al. 1995. Br J Pharmacol. 114: 6-7. PMID: 7712030
  10. Effect of a new aminopeptidase P inhibitor, apstatin, on bradykinin degradation in the rat lung.  |  Prechel, MM., et al. 1995. J Pharmacol Exp Ther. 275: 1136-42. PMID: 8531074
  11. Influence of several peptidase inhibitors on the pro-inflammatory effects of substance P, capsaicin and collagenase.  |  Damas, J., et al. 1996. Naunyn Schmiedebergs Arch Pharmacol. 354: 662-9. PMID: 8938667
  12. Inhibition of both aminopeptidase P and angiotensin-converting enzyme prevents bradykinin degradation in the rat coronary circulation.  |  Erşahin, C. and Simmons, WH. 1997. J Cardiovasc Pharmacol. 30: 96-101. PMID: 9268227
  13. Intravascular and interstitial degradation of bradykinin in isolated perfused rat heart.  |  Dendorfer, A., et al. 1997. Br J Pharmacol. 122: 1179-87. PMID: 9401784

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Apstatin, 1 mg

sc-201309
1 mg
$132.00

What is the shelf life of this product and has it's long-term stability been tested?

Asked by: jsc59
Thank you for the question. We provide a one year warranty for this product starting from the shipping date. Long-term stability has not been evaluated, yet.
Answered by: Technical Support Europe
Date published: 2018-01-09
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Rated 5 out of 5 by from WolfrumWolfrum, S. et al. (PubMed 11564655) reported that Apstatin, a selective inhibitor of aminopeptidase P, reduces myocardial infarct size by a kinin-dependent pathway. -SCBT Publication Review
Date published: 2015-03-28
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Apstatin is rated 5.0 out of 5 by 1.
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