Renin Inhibitor

Renin-IN-3 (Example 10) is a Renin inhibitor. Renin-IN-3 can be sued for hypertension research.

Aliskiren-d₆ (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC₅₀ of 1.5 nM.

PD 132002 is an orally active, potent renin inhibitor. PD 132002 weakly inhibits pepsin. PD 132002 produces substantial reductions in blood pressure.

CP 71362 is a renin inhibitor, a highly potent substrate-analog transition state mimic with antihypertensive properties. CP 71362 exhibits significant inhibitory activity against plasma renin from rats, dogs, and humans (IC₅₀ values are 3 nM, 0.0033 nM, and 20 nM, respectively). CP 71362 reduces the mean arterial pressure of anesthetized and conscious sodium-depleted animals in a dose-dependent manner, and has pharmacokinetic characteristics of rapid elimination and short duration of action. CP 71362 can be used in research related to hypertension and congestive heart failure.

Bucumolol is an orally active β-adrenergic receptor blocker. Bucumolol inhibits Renin release. Bucumolol exhibits activities including local anesthesia, antiarrhythmia, antihypertension, heart rate reduction, negative inotropy, cardiac action potential inhibition, and action potential duration shortening. Bucumolol does not increase cardiac electrical threshold, prolong atrial refractory period, or affect body weight in rodents. Bucumolol can be used in research related to arrhythmia and hypertension.

CP-69799 is an azahomostatine-containing oligopeptide transition-state analogue inhibitor with a hog renin IC₅₀ of 6e-9 M, human plasma renin IC₅₀ of 3e-7 M and K_i of 0.310 μM, and endothiapepsin K_i of 0.27 μM. CP-69799 binds endothiapepsin’s active site cleft in extended conformation, fills S4 to S3' pockets, displaces native solvent molecules, induces domain rotation, and reduces thermal mobility of endothiapepsin’s flap and helix regions. CP-69799 acts as a transition-state analogue inhibitor of hog renin and human plasma renin. CP-69799 contains a polar lysine residue at the P2' position, with a nitrogen atom replacing the P1' Cα atom of the hydroxyethylene dipeptide isostere. CP-69799 can be used for the research of hypertension.

A-74273 is an orally active peptide renin inhibitor (IC₅₀=3.1 nM). A-74273 competitively binds to the active site of renin, preventing angiotensinogen from being converted to ANG-I, thereby reducing the level of angiotensin II. A-74273 can be used in the study of diseases such as hypertension.

Renin inhibitor-1 (compound 26) is a potent and orally active renin inhibitor with IC₅₀s of 0.9, 1.8 nM for rh-renin and hPRA, respectively. Renin inhibitor-1 shows antihypertensive efficacy. Renin inhibitor-1 has the potential for the research of hypertension and cardiovascular/renal diseases.

PD 125967 is an oligopeptide renin inhibitor. PD 125967 can be used to low blood pressure.

Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC₅₀ values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension.

U 70714E is a Renin inhibitor with an IC₅₀ of 3.0 nM. U 70714E is used for the research of renin-related hypertension.

U 77436 is a Renin inhibitory peptide. U 77436 is used in the research of hypertension.

Aliskiren (Standard) is the analytical standard of Aliskiren. This product is intended for research and analytical applications. 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.

SR 43845 is a renin inhibitor. SR 43845 decreases blood pressure and inhibits plasma renin activity. SR 43845 can be used for hypertension research.

PD-134672 (CI-992) is a renin inhibitor containing a 2-amino-4-thiazolyl substituent. PD-134672 potently inhibits monkey renin in vitro and only weakly inhibits the related aspartic protease bovine feline hepsin D. The compound exhibits oral hypotensive activity in hyperreninemic normotensive monkeys. Based on its superior efficacy and long-lasting effects in vitro and in the normotensive macaque model, PD-134672 was selected for further evaluation in renal hypertensive monkeys.

KRI-1177 is a competitive, dipeptide human renin inhibitor with a K_i of 0.7 μM and an IC₅₀ of 90 nM. The IC₅₀ of KRI-1177 targeting cynomolgus monkey renin is 680 nM. KRI-1177 acts as an antihypertensive agent, angiotensin inhibitor and plasma renin activity inhibitor, which reduces systemic blood pressure and plasma angiotensin concentration. KRI-1177 exhibits a relatively long-lasting antihypertensive effect in cynomolgus monkeys and can be used for hypertension research.

WJM590 is an orally active antimalarial agent that also exhibits inhibitory activities against renin, cathepsin D, BACE1, and plasmodial aspartic proteases. WJM590 inhibits substrate and protein maturation processing mediated by key proteases of Plasmodium falciparum, arrests asexual blood-stage parasites at the late schizont stage, inhibits merozoite release, and blocks malaria parasite transmission via vectors. WJM590 exerts selective inhibitory activity against multiple Plasmodium species and drug-resistant Plasmodium falciparum strains, and reduces parasitemia in infected mice. WJM590 can be used in malaria-related research.

EMD 52297 is a Renin inhibitor, with acute hemodynamic and hormonal effects. EMD 52297 also acts as an ACE inhibitor.

Renin inhibitory peptide, statine is an inhibitor of Renin. Renin inhibitory peptide, statine inhibits the plasma renin activity of human plasma renin, porcine renin, and sodium-depleted conscious dogs. Renin inhibitory peptide, statine reduces the mean arterial pressure of sodium-depleted conscious dogs, induces a sustained, dose-dependent decrease in blood pressure, and triggers a maximum hypotensive response. Renin inhibitory peptide, statine can be used in hypertension-related research.

A-65317 is a primate-selective renin dipeptide inhibitor (IC₅₀ of 0.37 nM) with long hypotensive response.