KALLISTOP®, Kallikrein inhibitor

Description
KALLISTOP™ a 4-amidinoanilide derivative of phenyl-2-aminobutyric acid is a relatively selective inhibitor of plasma kallikrein (PK). The inhibitory effect depends on the pH-value. It is increased below pH 7.0 and is decreased above pH 8.0.

Chemistry
Structural formula:
 
Formula: C₂₄H₂₆N₄0₃S • HCI
MW: 487.0
Chemical name: 2-Tosyl-(D,L)-homophenyl-alanine-4-amidinoanlde hydrochloride
Purity: 99.9 % as determined by HPLC
Solubility: readily soluble in organic solvents (methanol, ethanol, DMSO), soluble in H₂0 and in aqueous buffers up to 4 mM.

Known Applications
KALLISTOP™ is employed to inhibit plasma kallikrein (PK) competitively.
KALLISTOP™ has been used in chromogenic assays for the determination of factor Xlla activity in plasma with a chromogenic substrate for Factor XIIa (H-D-HHT-Gly-Arg-pNA). KALLISTOP™ suppresses undesired cleavage of the substrate by plasma kallikrein. ^[2]

Inhibitory Activity
Ki constants: The following table shows the inhibition of different serine proteinases.
Enzyme   
Trypsin: 1.3 Ki [µM]
Thrombin: 170 Ki [µM]
Factor Xa: 31 Ki [µM]
Factor XIIa: 100 Ki [µM]
Plasmin: 10 Ki [µM]
Urokinase: 17 Ki [µM]
Two chain tPA: 36 Ki [µM]
Plasma Kallikrein: 0.7 Ki [µM]
Glandular Kallikrein: 100 Ki [µM]
Batroxobin (B. atrox): 5.7 Ki [µM]
Batroxobin (B. moojeni): 11.7 Ki [µM]
PCa: 79 Ki [µM]
Tryptase: 12 Ki [µM]

Presentation
Screw-capped amber glass vial containing 5 mg of lyophilized inhibitor. Solubility in 1% DMSO/water:
≥ 2 mg/mL.

Storage
Store at 2 - 8 °C. It is recommended to aliquote the inhibitor, avoid freeze-thaw cycles.

Category: Research use only

Type: Inhibitor

Product Availability: Worldwide

Manufacturer: ImmBioMed GmbH & Co KG, Germany

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