Cardiovascular Disease

Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (I_Na and I_Kr with IC₅₀ values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor. Antianginal agent.

Chlorothiazide is an orally active diuretic and anti-hypertensive agent.

Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases.

Triamterene blocks epithelial Na⁺ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene is an inhibitor of the TGR5 receptor.

CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a K_i of 12.8 nM.

GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.

TY-52156 is a potent and selective S1P₃ receptor antagonist with a K_i value of 110 nM.

Labetalol (AH5158) hydrochloride is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol hydrochloride is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol hydrochloride can be used in the study of cardiovascular diseases, such as hypertension during pregnancy.

Atipamezole (MPV 1248) is a potent α₂-adrenoceptor antagonist with a K_i of 1.6 nM.

(S)-(-)-Bay-K-8644 is an agonist of L-type Ca²⁺ channel. (S)-(-)-Bay-K-8644 activates Ba²⁺ currents (I_Ba) (EC₅₀=32 nM).

Aflibercept (VEGF Trap) is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease.

Metoprolol tartrate is an orally active, selective β1-adrenoceptor antagonist. Metoprolol tartrate shows anti-inflammation, antitumor and anti-angiogenic properties.

Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC₅₀ value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC₅₀ values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS).

Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT₂ receptor, with an IC₅₀ of 0.9 nM, less active on Histamine H₁, Dopamine D₂, Adrenergic α₁, Adrenergic α₂ receptors.

Fondaparinux sodium is an antithrombin-dependent factor Xa inhibitor.

Ripasudil (K-115) is a specific inhibitor of ROCK, with IC₅₀s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

Diltiazem hydrochloride is a Ca²⁺ influx inhibitor (slow channel blocker or calcium antagonist).

IWP-4 is a Wnt inhibitor with an IC₅₀ of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC₅₀ of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC₅₀ = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure.

Guanfacine hydrochloride is an orally active and blood-brain barrier permeability noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD).

Latanoprost (PHXA41) is a prostaglandin F2α analogue and can be used for glaucoma research. Latanoprost can effectively pass through cornea and be hydrolyzed by esterase to latanoprost acid. latanoprost acid is an F-prostaglandin (FP) receptor agonist, and can effectively reduce intraocular pressure (IOP) by increasing the outflow of aqueous humor through uvea.