A competitive inhibitor of serine proteases; inhibits human thrombin

Gabexate (mesylate) – 10 mg

Brand:
Cayman
CAS:
56974-61-9
Storage:
-20
UN-No:
Non-Hazardous - /

Gabexate is a competitive inhibitor of serine proteases that inhibits human thrombin, urokinase, plasmin, and Factor Xa (Kis = 0.97, 1.3, 1.6, and 8.5 μM, respectively).{40664},{40665} It also inhibits bovine thrombin, Factor Xa, and trypsin, and porcine plasma kallikrein (Kis = 1.4, 2.1, 2.6, and 0.2 μM, respectively).{40664},{40666} In vitro, gabexate inhibits clotting activity of thrombin (IC50 = 10 μM).{40664} In vivo, it inhibits fibrin formation in rats when administered at a continuous infusion of 120 μmol/kg per hour.{40667} Gabexate inhibits LPS-stimulated TNF-α production from monocytes by inhibiting binding of NF-κB and activator protein 1 (AP-1) to target sites and inducing degradation of IκBα.{40668}  

 

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SKU: 23767 - 10 mg Category:

Description

A competitive inhibitor of serine proteases; inhibits human thrombin, urokinase, plasmin, and Factor Xa (Kis = 0.97, 1.3, 1.6, and 8.5 μM, respectively); inhibits bovine thrombin, Factor Xa, and trypsin, and porcine plasma kallikrein (Kis = 1.4, 2.1, 2.6, and 0.2 μM, respectively); inhibits clotting activity of human thrombin (IC50 = 10 μM); inhibits fibrin formation in rats (continuous infusion of 120 μmol/kg per hour)

Formal name: 4-[[6-[(aminoiminomethyl)amino]-1-oxohexyl]oxy]-benzoic acid ethyl ester, monomethanesulfonate

Synonyms: 

Molecular weight: 417.5

CAS: 56974-61-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Blood Coagulation Factors||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cardiovascular System|Blood|Coagulation & Hemostasis||Research Area|Cardiovascular System|Blood|Thrombosis||Research Area|Immunology & Inflammation|Innate Immunity

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