Cardiovascular Disease

Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC₅₀ values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.

Pitavastatin (NK-104) sodium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin sodium inhibits cholesterol synthesis from acetic acid with an IC₅₀ of 5.8 nM in HepG2 cells. Pitavastatin sodium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin sodium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.

Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial 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.

Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.

Zalunfiban (RUC-4) acetate is a potent, selective platelet αIIbβ3antagonist (IC₅₀=45 nM). Zalunfiban acetate can be used for the research of myocardial infarction (MI).

Fluvastatin (XU 62-320) sodium monohydrate is a first fully synthetic, competitive HMG-CoA reductaseinhibitor with an IC₅₀ of 8 nM. Fluvastatin (sodium monohydrate) protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.

Mibefradil dihydrochloride hydrate (Ro 40-5967 dihydrochloride hydrate) is a effectively long-acting calcium channel antagonist, used as an antihypertensive agent. Mibefradil dihydrochloride hydrate acts via a higher affinity block for low-voltage-activated (T) than for high-voltage-activated (L) calcium channels.

Fosinopril (SQ28555 free acid) is the ester proagent of angiotensin-converting enzyme (ACE) inhibitor with an IC₅₀ value of 0.18 μM. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with an K_i value of 1.675 μM.

(S)-(-)-Propranolol is the active isomer of Propranolol (HY-B0573B), with 98-fold greater activity than (R)-(+)-Propranolol. (S)-(-)-Propranolol produces antinociception-related phenotypes in mouse models, accompanied by sedative and ataxic side effects. (S)-(-)-Propranolol can be used in research related to hypertension, myocardial infarction, and pain.

Cangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist.

Sotalol is an orally active, non-selective β-adrenergic receptor blocker. Sotalol is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent.

Blonanserin dihydrochloride is a potent and orally active 5-HT_2A and dopamine D2 receptor antagonist, with K_i values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator.

Amiodarone hydrochloride solution is mainly composed of Amiodarone hydrochloride (HY-14188). Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) tails with an IC₅₀ of ∼45 nM. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias.

Indimilast is a PDE4 inhibitor. Indimilast is used for research on dyslipidemia and related diseases.

Tedixaban (Tedixabanum) is a Factor Xa inhibitor and anticoagulant with an IC₅₀ of 0.50 nM. Tedixaban is applicable to research on thrombosis-related complications.

PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC₅₀ of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC₅₀s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity.

Bumetanide sodium, a highly potent loop diuretic, is a Na⁺-K⁺-Cl⁺ cotransporter (NKCC) blocker. Bumetanide sodium is a selective NKCC1 inhibitor, and also inhibits NKCC2, with IC₅₀s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.

ASP7967 hemifumarate is an orally active ligand of the RNA aptamer AC17-4 with a K_d of 12 nM. ASP7967 hemifumarate binds AC17-4 to regulate aptazyme-based and exon-skipping riboswitches, thereby enabling small-molecule-controlled transgene expression without exogenous protein factors. ASP7967 hemifumarate can be used for the study of synthetic RNA switches, gene expression regulation and AAV-based gene therapy-related expression control.