RXPA 380

Names

[ Name ]:
RXPA 380

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Angiotensin-converting Enzyme (ACE)

[Target]

Ki: 3 nM (C-terminal ACE), 10 μM (N-terminal ACE)[1] IC50: 2.5 nM (C-domain mutants of human recombinant ACE), 10 μM (N-domain mutants of human recombinant ACE)[1]

[In Vitro]

RXPA 380 shows Ki(app) values of 12 nM and 12 μM for the C- and N-domain of mouse somatic ACE[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₃H₃₆N₃O₇P

[ Molecular Weight ]:
617.63

Related Compounds

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