Aliskiren fumarate

Aliskiren fumarate is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren fumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1][2][3].

Research Areas >> Cancer

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> Metabolic Enzyme/Protease >> Renin

IC50: 1.5 nM (renin)[1]

Aliskiren fumarate (< 10 mg/kg, Orally, daily) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[2]. Aliskiren fumarate (10 mg/kg, Intragastrically, once) significantly alleviates multiple cachexia‑associated symptoms in BALB/c mice bearing C26 mouse colon carcinoma cells, including BW loss, tumor burden, muscle wasting, muscular dysfunction, and shortened survival[3].

[1]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758

[2]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705.

[3]. Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36(5):3014-3022.