Renin Inhibitor

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

Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC₅₀ of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.

Sodium new houttuyfonate (SNH) is a partially reversible NDM-1 inhibitor with an IC₅₀ of 14.2 μM. Sodium new houttuyfonate is an inhibitor against renin and angiotensin I converting enzyme (ACE). Sodium new houttuyfonate can recover the antibacterial activity of Meropenem (HY-13678) against E. coli BL21/pET15b-blaNDM-1.

Theasinensin C is an orally effective renin inhibitor and gut microbiota modulator, with an IC₅₀ of 40.21 μM against renin activity. Theasinensin C selectively enriches Akkermansia muciniphila in the gut microbiota, enhances the Akkermansia muciniphila-mediated hydrolysis of the PTS domain of mucin, drives the accumulation of luminal glutamine and serine, and regulates the gut-kidney-liver glutamine/serine metabolic signaling pathway to promote creatine biosynthesis. Theasinensin C improves cognitive function, reduces pro-inflammatory cytokines, alleviates neuropathological changes and restores intestinal barrier integrity. Theasinensin C can be used in research related to hypertension and neuroinflammation induced by high-fructose diet.

Lyciumin D acts as an angiotensin-converting enzyme inhibitor and renin inhibitor. Lyciumin D can be used for the research of hypertension.

Renin IN-2 (compound 27) is an orally active human renin inhibitor with an IC₅₀ of 0.059 μM. Renin IN-2 can be used in the research of hypertension.

Araloside A (Chikusetsusaponin IV), triterpenoid saponins, is an orally active component of Aralia elata. Araloside A shows low-renin-inhibitory activity with an IC₅₀ of 77.4 μM. Araloside A can inhibit cell proliferation and induce apoptosis. Araloside A suppresses inflammatory cytokines IL-1β and IL-6 production. Araloside A can be used for the researches of cancer, inflammation and cardiovascular disease, such as renal cell carcinoma and rheumatoid arthritis.

Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a proagent of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research.

VTP-27999 TFA is an alkyl amine Renin inhibitor; VTP-27999 TFA is useful for Hypertension and End-Organ Diseases.

SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC₅₀=0.4 nM, human plasma renin activity IC₅₀=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research.

VTP-27999 Hydrochloride is an orally active renin inhibitor. VTP-27999 Hydrochloride functionally inhibits renin and acid-activated prorenin, suppresses plasma renin activity and modulates plasma and urinary aldosterone levels. VTP-27999 Hydrochloride reduces mean arterial blood pressure, induces plasma renin concentration increases, decreases plasma angiotensin II levels and enhances renin immunoreactivity. VTP-27999 (Hydrochloride) can be used for the research of hypertension and chronic renal disease.

Lyciumin A, a cyclic octapeptide, exhibits inhibitory activity on proteases, renin and angiotensin-converting enzyme. Lyciumin A can be used for the research of hypertension.

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.

Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride is an orally active and selective renin inhibitor, with IC₅₀ of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases and cancer cachexia^-.

Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol fumarate is a proagent of Pindolol (HY-B0982). Bopindolol fumarate can be used for essential and renovascular hypertension research.

Zankiren (A-72517) is an orally active inhibitor for renin. Zankiren exhibits renal vasodilator effect, through reduction of angiotensin II formation without affecting other vasodilator mechanisms.

Imarikiren hydrochloride is a renin inhibitor. Imarikiren hydrochloride can be used for the study of cardiovascular and renal diseases such as hypertension, heart failure, and diabetic nephropathy by blocking the renin-angiotensin (RA) system.

SQ 32970 is a tripeptidic renin inhibitor. SQ 32970 potently inhibits endothia protease.

SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 μmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 μmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 μmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.

SQ 33800 is a potent inhibitor of human renin with an IC₅₀ of 0.35 nM. SQ 33800 can be used for the research of cardiovascular disease.