CGS 35066 (CAS 261619-50-5)

CGS 35066 is a a potent endothelin-converting enzyme (ECE) inhibitor. When compared to neutral endopeptidase 24.11, it displays > 100-fold selectivity (IC50 values are 22 and 2300 nM respectively). Another interesting property of CGS 35066 is that it blocks the hypertensive effects induced by big ET-1 n vitro and is able to reduce the magnitude of cerebral vasospasm following subarachnoid hemorrhage (SAH).

Literaturhinweise

De Lombaert et al (2000) Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action. J.Med.Chem. 43 488. Trapani et al (2000) Pharmacological properties of CGS 35066, a potent and selective endothelin-