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Aliskiren hydrochloride is a direct renin inhibitor with an IC50 = 0.72 nM. Renin is the first enzyme in the renin-angiotensin-aldosterone system (RAAS) and cleaves angiotensinogen, an inactive peptide, into angiotensin I. Inhibition of renin prevents this cleavage and subsequent activiation of angiotensin II receptors.
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