Pefabloc TH (a-NAPAP)

Catalogue Number: 381-01
Size: 5 x 1 mg

A synthetic specific Thrombin inhibitor.

The benzamidine moiety is a key structure for the development of inhibitors of trypsin-like enzymes. It mimics the protonated side-chain of the basic amino acids Arg and Lys which is hydrolysed by these enzymes. Pefabloc TH (a-NAPAP) is one of the most potent and selective competitive inhibitors of thrombin.

Pefabloc TH can be used in diagnostic systems, analytical applications, research and industrial purification processes to exclude undesired thrombin activity. It can also be used as a potent anticoagulant in in vitro test systems.

Chemical Formula: C₂₇H₃₁N₅O₄S . AcOH

Identity: N-a-(2-naphthylsulphonylglycyl)-4-amidino-(D,L)-phenylalanine piperidide acetate salt

Molecular Weight: 581.7

Ki values for the inhibition of several trypsin-like serine proteases by Pefabloc TH

Enzyme	Ki [µM]
Trypsin	0.69
Thrombin (bovine)	0.006
Factor Xa	7.9
Factor XIIa	450
Plasmin	30
uPA	230
sc-tPA	430
tc-tPA	70
Plasma kallikrein	14.4
Glandular kallikrein	93
Acrosin	2.9
Batroxobin (B. atrox)	1.7
Batroxobin (B. moojeni)	3.8
PCa	4.8
Tryptase	45
Chymotrypsin	625

References

Stürzebecher J, Walsmann P, Voigt B, Wagner G. Inhibition of bovine and human thrombins by derivatives of benzamidine. Thromb Res 1984; 36: 457-65.

Certificates
Certificate of Analysis (381-01 PEFABLOC TH (a-NAPAP))

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Pefabloc TH (a-NAPAP)

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