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Chemical Compound Review

Declaben     2-chloro-4-(1- hydroxyoctadecyl)benzoic acid

Synonyms: LODELABEN, Lodelabenum, SureCN636150, CHEMBL2105119, LS-36505, ...
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Disease relevance of SC 39026

  • Failure to inhibit medial hypertrophy with SC-39026 suggests that a different mechanism or a different elastase may be involved in this structural change [1].
  • SC-39026 did not significantly reduce monocrotaline-induced medial hypertrophy of muscular arteries, endothelial injury, and associated subendothelial edema; nor was there a significant increase in the proportion of the medial elastin, although a trend was apparent [1].
  • SC-39026 is inactive against hog pancreatic elastase, bovine alpha-chymotrypsin and Pseudomonas aeruginosa elastase, but does inhibit human neutrophil cathepsin G with an IC50 of approximately 2.5 microM [2].
  • SC-39026 reduced the number of muscularized arteries and the level of pulmonary arterial pressure during exposure to chronic hypoxia [3].
  • Our previous studies showed that increased pulmonary artery elastolytic activity is associated with monocrotaline-induced pulmonary hypertension in rats, and the latter is reduced by the elastase inhibitor SC-39026 [4].

High impact information on SC 39026

  • In contrast, monocrotaline-injected rats given SC-39026 had significantly lower mean pulmonary artery pressure than those given vehicle (21.0 +/- 1.6 vs. 27.5 +/- 0.8 mm Hg, p less than 0.05), and this correlated with a significant reduction in the number of abnormally muscularized arteries at alveolar wall level (r2 = 0.89, p less than 0.001) [1].
  • ICI-200,880, a competitive slow-binding elastase inhibitor, was significantly less potent to inhibit A alpha(1-21), having an IC50 of 75 microM, while Declaben, a reversible noncompetitive inhibitor, was inactive at concentrations as great as 200 microM [5].
  • SC-39026, (+/-) 2-chloro-4-(1-hydroxyoctadecyl)benzoic acid, inhibits human neutrophil elastase with an IC50 of 0.5 microM (KI of 1.5 microM) [2].
  • Neutrophil elastases isolated from rat, hamster, rabbit and hog are also inhibited by SC-39026 [2].
  • Previously in rats injected with the toxin monocrotaline and administered SC-39026, a serine elastase inhibitor, pulmonary hypertension was decreased in association with reduced muscularization of peripheral pulmonary arteries [3].

Gene context of SC 39026


  1. SC-39026, a serine elastase inhibitor, prevents muscularization of peripheral arteries, suggesting a mechanism of monocrotaline-induced pulmonary hypertension in rats. Ilkiw, R., Todorovich-Hunter, L., Maruyama, K., Shin, J., Rabinovitch, M. Circ. Res. (1989) [Pubmed]
  2. SC-39026, a specific human neutrophil elastase inhibitor. Nakao, A., Partis, R.A., Jung, G.P., Mueller, R.A. Biochem. Biophys. Res. Commun. (1987) [Pubmed]
  3. Chronic hypoxic pulmonary hypertension in rats and increased elastolytic activity. Maruyama, K., Ye, C.L., Woo, M., Venkatacharya, H., Lines, L.D., Silver, M.M., Rabinovitch, M. Am. J. Physiol. (1991) [Pubmed]
  4. Inhibition of elastolysis by SC-37698 reduces development and progression of monocrotaline pulmonary hypertension. Ye, C.L., Rabinovitch, M. Am. J. Physiol. (1991) [Pubmed]
  5. Formation of polymorphonuclear leukocyte elastase: alpha 1 proteinase inhibitor complex and A alpha (1-21) fibrinopeptide in human blood stimulated with the calcium ionophore A23187. A model to characterize inhibitors of polymorphonuclear leukocyte elastase. Pacholok, S.G., Davies, P., Dorn, C., Finke, P., Hanlon, W.A., Mumford, R.A., Humes, J.L. Biochem. Pharmacol. (1995) [Pubmed]
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