| Hazard Information | Back Directory | [Description]
RXPA380 is a potent and highly selective inhibitor of the angiotensin-converting enzyme C-domain. | [Uses]
RXPA 380 is a C-terminal specific angiotensin-converting enzyme (ACE) inhibitor with a Ki of 3 nM. RXPA 380 inhibits C-domain mutants of human recombinant ACE with an IC50 of 2.5 nM[1]. | [in vivo]
RXPA 380 (0.9-30 mg/kg; i.v.; once) inhibits ACE activity in mice[1]. | Animal Model: | Male C57BL6/J mice[1] | | Dosage: | 0.9, 3, 10, and 30 mg/kg | | Administration: | Intravenous infuse for 30 minutes | | Result: | Induced a dose-dependent decrease of the Ang II/Ang I ratio. Blocked the cleavage of exogenously administered bradykinin. |
| [References]
[1] Georgiadis D, et al. Roles of the two active sites of somatic angiotensin-converting enzyme in the cleavage of angiotensin I and bradykinin: insights from selective inhibitors. Circ Res. 2003 Jul 25;93(2):148-54. DOI:10.1161/01.RES.0000081593.33848.FC |
|
|