Cardiovascular Disease

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.

Cariporide is a Na+/H+ Exchanger 1 (NHE-1) inhibitor. Cariporide inhibits the expression of monocyte endothelial cell adhesion and intercellular adhesion molecule-1 (ICAM-1) mediated by high glucose (HG) by inhibiting the activation of NHE-1.

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.

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).

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

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.

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.

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.

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.

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.

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.

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.

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.

(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.

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.

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

Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a K_i of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a K_i of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.

Levosimendan solution is mainly composed of Levosimendan (HY-14286). Levosimendan (Simsndan; OR-1259) is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.

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.