Cardiovascular Disease

Regrelor (INS50589 (free acid)) is a selective, reversible, and competitive P2Y12 receptor antagonist and an adenosine 5′-monophosphate derivative. Regrelor inhibits ADP (HY-W010918)-induced aggregation of human washed platelets with an IC₅₀ of 0.016 μM. Intravenous infusion of Regrelor rapidly and dose-dependently inhibits ADP-induced platelet function, and platelet function gradually recovers after cessation of infusion. Regrelor can be used for research on P2Y12-mediated platelet function and cardiovascular regulation.

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.

P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC₅₀ value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease.

Mecobalamin solution is mainly composed of Methylcobalamin (HY-B0586). Methylcobalamin (CH3-B12), a cobalamin, is a form of vitamin B12 and can be used in research related to peripheral neuropathy or megaloblastic anemia caused by a deficiency of vitamin B12.

β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC₅₀=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).

PD151242 is a selective competitive antagonist of the endothelin ET_A receptor, with K_D values of 0.65 nM, 0.64 nM and 1.92 nM for human, rat and porcine receptors, respectively, and a K_D value of 104 μM for the human ET_β receptor. When radiolabeled as [¹²⁵I]-PD151242, PD151242 can be used to visualize and localize renal vascular ET_A receptors.

Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC₅₀ of 62.23 nM. Antianemia agent.

DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC₅₀ of 11 nM.

CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC₅₀s of 0.002 μM and 0.06 μM, respectively.

Niacin (Vitamin B3; Nicotinic acid) hydrochloride is an orally active B3 vitamin that is an essential nutrient for humans. Niacin hydrochloride plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin hydrochloride is also used in the study of cardiovascular diseases.

Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.

Fenoldopam (SKF 82526) hydrochloride is a D₁ receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC₅₀=0.8974 μM). Fenoldopam hydrochloride shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis.

Methoxamine is a selective alpha1-adrenergic receptor agonist. Methoxamine causes vasoconstriction and increased peripheral vascular resistance. Methoxamine hydrochloride significantly increased the overflow of ATP, ADP and AMP, but not adenosine, by a prazosin-sensitive mechanism in the rabbit pulmonary artery.

P2Y1 antagonist 6 (Example 30) is a P2Y1 receptor (P2Y1 Receptor) antagonist and can be used in antithrombotic research.

BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC₅₀ of 7.3 nM and a K_i of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.

Mito-Esculetin (Mito-Esc) is an orally active mitochondria-targeted derivative of Esculetin (HY-N0284). Mito-Esculetin inhibits LPS-induced phosphorylation of STAT3 Tyr-705, partially reverses LPS-mediated depletion of SIRT3, and enhances the AMPK-SIRT1 signaling axis. Mito-Esculetin inhibits PAI-1 activity, regulates miRNA, and induces phosphorylation of IRS and AKT. Mito-Esculetin suppresses oxidant-induced endothelial dysfunction, Ang-II (HY-13948)- and high glucose-induced atherosclerotic plaque formation, Palmitate (HY-N0830)-induced insulin resistance, as well as high glucose-mediated endothelial cell senescence and inflammatory responses. Mito-Esculetin reduces body weight and non-esterified fatty acid (NEFA) levels. Mito-Esculetin can be used in research related to acute coronary syndrome, type 2 diabetes, and hyperglycemia-induced atherosclerosis.

(R)-Efonidipine ((R)-NZ-105) is an orally active, selective T-type Ca²⁺ channel blocker. (R)-Efonidipine does not inhibit high-voltage-activated Ca²⁺ channels, voltage-dependent Na⁺ channels, or Ca²⁺-activated K⁺ channels. (R)-Efonidipine modulates cardiac autonomic function by increasing parasympathetic activity and decreasing sympathetic activity. (R)-Efonidipine significantly improves survival in a mouse model of dilated cardiomyopathy. (R)-Efonidipine can be used in research on ischemic encephalopathy, heart failure, and hypertension.

FIPI hydrochloride is a phospholipase D (PLD) inhibitor with an IC₅₀ for PLD1 and PLD2 of about 25 nM. FIPI hydrochloride regulates cytoskeletal recombination, cell diffusion and chemotaxis. FIPI hydrochloride can be used in cancer research. In addition, FIPI hydrochloride can enhance the secretion and aggregation of platelet dense particles, inhibit thrombosis, reduce ischemic stroke infarct volume and improve nerve function.

Anagliptin (SK-0403) hydrochloride is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC₅₀ of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC₅₀s of 68 nM and 60 nM, respectively.

Cassaine (Nervocidine) is a Na⁺/K⁺-ATPase inhibitor. Cassaine stabilizes phosphorylated intermediates, slows spontaneous dephosphorylation and blocks potassium-stimulated dephosphorylation. Cassaine exhibits non-competitive inhibition with respect to K⁺, shows inhibition enhanced by Pi and antagonized by Na⁺. Cassaine induces positive inotropic effects in perfused hearts with faster inotropy offset. Cassaine can be used for research on cardiac arrhythmias.