SYNTHETIC REVERSIBLE INHIBITORS

Cat Num.ProductMW(Da)FormulationSize
9-DAPA

Dansylarginine N-(3-ethyl-1.5-pentanediyl)amide•HCl

539Dansylarginine; N-(3-ethyl-1.5-pentanediyl)amide; HCl1 mg
8-099-11

Pefabloc® FG

Pefabloc® FG inhibits disturbing fibrin-related turbidity, gel formation and fibrin formation during purification and processing of clotting factors and other plasma proteins.

485.5H-Gly-Pro-Arg-Pro-OH; AcOH1 x 50 mg
8-099-01

Pefabloc® FG

485.5H-Gly-Pro-Arg-Pro-OH; AcOH1 g
8-381-01

Pefabloc® TH

Potent and selective competitive inhibitors of thrombin.

581.7N-α-(2-naphthylsulfonylglycyl)-4-amidino-(D, L)-phénylananine pipéridide acétate (NAPAP)5 mg
8-382-03

Pefabloc® uPA

Low molecular weight synthetic inhibitor for urokinase (uPA).

650.3N-α-(2,4,6-triisopropyl-phenylsulfonyl)-3-amidino-(L)- phenylananin-4-ethoxycarbonyl-piperazid hydrochloride5 mg
8-391-03

Pefabloc® tPA/Xa

445.42,7-Bis(4-Amidinobenzylidene)-cycloheptanone-(1) dihydrochloride5 mg
8-398-01

Pefabloc® SP

Pefabloc® SP can be used to inhibit the proteolytic activity of trypsin-like serine proteinases during purification of polypeptides and proteins. Due to its low molecular weight, the separation from the protein of interest can be easily accomplished by conventional techniques. Pefabloc® SP inhibits serine proteinases competitively.
The inhibitory effect depends on the pH-value. It is increased below pH 7.0 and is decreased above pH 8.0.

242.74-amidinophenylpyruvic acid hydrochloride0.5 g
8-380-03

Pefabloc® PK

Pefabloc® PK inhibits plasma kallikrein (PK) competitively and suppresses undesired cleavage of the substrate by plasma kallikrein.

4872-Tosyl-(D,L)-homophenylalanine-4-amidinoanilide hydrochloride5 mg
8-383-03

Pefabloc® PL

Low molecular weight synthetic inhibitor for plasmin.

640.2Nα-(2-Naphthylsulfonyl)-3-amidino-(D,L)-phenylalanyl-nipecotic acid-thiophene-2-methylamide hydrochloride5 mg
8-385-03

Pefabloc® Xa

To exclude undesired activity of factor Xa in the presence of other serine proteases.

469Nα-Tosylglycyl-3-amidino-(D,L)-phenylalanine-methylester hydrochloride5 mg


Inhibition constants Ki in μM of Pefabloc inhibitors
for serine proteinases

Description


Detection and determination of proteinases, studies on their interactions with substrates and effectors and the investigation of their physiological role are greatly facilitated by the use of proteinase inhibitors.
In this context, especially synthetic, low-molecular weight inhibitors of different selectivity are very useful. They are widely applied during purification and characterization of proteinases.
Furthermore, synthetic inhibitors are useful tools for suppression of undesired proteolytic activity. Depending upon the manner in which the inhibitor is attached to the enzyme, one distinguishes reversible and irreversible inhibitors.

Characteristics


Pentapharm offers a selection of inhibitors derived from benzamidine. They can help in the characterization of trypsin-like enzymes.
Most Pefablocs® exhibit a selective inhibitory activity on certain trypsin-like proteinases of physiological relevance. However, each inhibitor will of course display a characteristic action on other serine proteinases (see table on Ki-values page 47).

Advantages


Supplied lyophilized or frozen
Expiry date > 1 year
Glass vial or plastic tubes
Discount according to quantities

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