Date published: 2026-2-13

1-800-457-3801

SCBT Portrait Logo
Seach Input

PKSI-527 (CAS 128837-71-8)

5.0(1)
Write a reviewAsk a question

See product citations (5)

Alternate Names:
trans-4-Aminomethylcyclohexanecarbonyl-phenylalanyl-4-carboxymethylanilide
Application:
PKSI-527 is a highly selective plasma kalikrein inhibitor that can be used for affinity purification of kalikrein
CAS Number:
128837-71-8
Purity:
≥95%
Molecular Weight:
473.99
Molecular Formula:
C25H31N3O4•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

QUICK LINKS

PKSI-527 is a highly selective plasma kallikrein inhibitor (Ki = 0.81 muM) which can be used for affinity purification of kalikrein. It suppresses collagen-induced arthritis in a mouse model. Additionally, PKSI-527 may act to synergize with NO donors producing antithrombotic effects. It also prolongs partial thromboplastin and euglobulin clot lysis times.


PKSI-527 (CAS 128837-71-8) References

  1. Amino acids and peptides. LIII. Synthesis and biological activities of some pseudo-peptide analogs of PKSI-527, a plasma kallikrein selective inhibitor: the importance of the peptide backbone.  |  Fukumizu, A., et al. 1999. Chem Pharm Bull (Tokyo). 47: 1141-4. PMID: 10478469
  2. Binding diversity of a noncovalent-type low-molecular-weight serine protease inhibitor and function of a catalytic water molecule: X-ray crystal structure of PKSI-527--inhibited trypsin.  |  Tomoo, K., et al. 2001. J Biochem. 129: 455-60. PMID: 11226886
  3. Isolation of plasma kallikrein by high efficiency affinity chromatography and its characterization.  |  Tada, M., et al. 2001. Biol Pharm Bull. 24: 520-4. PMID: 11379773
  4. Suppression of argatroban-induced endogenous thrombolysis by PKSI-527, and antibodies to TPA and UPA, evaluated in a rat arterial thrombolysis model.  |  Hashimoto, M., et al. 2003. Thromb Haemost. 89: 820-5. PMID: 12719778
  5. Synthesis of trans-4-aminomethylcyclohexanecarbonyl-L- and -D-phenylalanine-4-carboxymethylanilide and examination of their inhibitory activity against plasma kallikrein.  |  Wanaka, K., et al. 1992. Chem Pharm Bull (Tokyo). 40: 1814-7. PMID: 1394697
  6. A finding of highly selective synthetic inhibitor of plasma kallikrein; its action to bradykinin generation, intrinsic coagulation and experimental DIC.  |  Okamoto, S., et al. 1992. Agents Actions Suppl. 38 (Pt 1): 198-205. PMID: 1466271
  7. Synergistic antithrombotic effect of a combination of NO donor and plasma kallikrein inhibitor.  |  Ikarugi, H., et al. 2005. Thromb Res. 116: 403-8. PMID: 16122553
  8. Development of selective inhibitors against plasma kallikrein.  |  Teno, N., et al. 1991. Chem Pharm Bull (Tokyo). 39: 2930-6. PMID: 1839246
  9. Angiotensin II type 2 receptor-mediated inhibition of norepinephrine release in isolated rat hearts.  |  Sasaoka, T., et al. 2008. J Cardiovasc Pharmacol. 52: 176-83. PMID: 18670361
  10. Predicting subsite interactions of plasmin with substrates and inhibitors through computational docking analysis.  |  Gohda, K., et al. 2012. J Enzyme Inhib Med Chem. 27: 571-7. PMID: 21992704
  11. Effect of a highly selective plasma-kallikrein synthetic inhibitor on contact activation relating to kinin generation, coagulation and fibrinolysis.  |  Wanaka, K., et al. 1990. Thromb Res. 57: 889-95. PMID: 2382257
  12. [Study on the expression of bradykinin and its receptors B1R and B2R in the kidney immune injury in trichloroethylene-sensitized mouse].  |  Wang, H., et al. 2015. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 33: 486-91. PMID: 26653642
  13. [Role of kallikrein kinin system activation in kidney injury induced by trichloroethylene sensitized mice].  |  Liu, M., et al. 2016. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 34: 184-8. PMID: 27220437
  14. Effects of a highly selective plasma kallikrein inhibitor on collagen-induced arthritis in mice.  |  Fujimori, Y., et al. 1993. Agents Actions. 39: 42-8. PMID: 8285139
  15. Effects of a highly selective synthetic inhibitor of plasma kallikrein on disseminated intravascular coagulation in rats.  |  Katsuura, Y., et al. 1996. Thromb Res. 82: 361-8. PMID: 8743731
  16. Purification method for human plasma kallikrein by a new affinity chromatography.  |  Tada, M., et al. 1998. Biol Pharm Bull. 21: 105-8. PMID: 9514601
  17. Design of plasma kallikrein inhibitors: functional and structural requirements of plasma kallikrein inhibitors.  |  Tsuda, Y., et al. 1998. Chem Pharm Bull (Tokyo). 46: 452-7. PMID: 9549887

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

PKSI-527, 5 mg

sc-222181
5 mg
$189.00

PKSI-527, 25 mg

sc-222181A
25 mg
$689.00