coronary artery

GP2-114 is a catecholamine exercise mimetic that can be used to study coronary artery disease (CAD).

Nebivolol hydrochloride (R 065824 hydrochloride) is a cardioselective ADRENERGIC BETA-1 RECEPTOR ANTAGONIST (beta-blocker) that functions as a VASODILATOR through the endothelial L-arginine/ NITRIC OXIDE system. It is used to manage HYPERTENSION and chronic HEART FAILURE in elderly patients.

Diaminohydroxypropanetetraacetic acid has been investigated for the treatment of Vascular Disease, Coronary Disease, Myocardial Ischemia, Coronary Restenosis, and Coronary Artery Disease, among others

Aspirin (Acetylsalicylic Acid) is a COX inhibitor that inhibits COX1 and COX2 (IC50=5 210 μg mL) with selective, irreversible, and oral activity. Aspirin is also a histone deacetylase inhibitor that up-regulates the cell cycle blocking protein, p21. Aspirin has a variety of activities. Aspirin has anti-inflammatory, antipyretic and analgesic, and antiplatelet aggregation activities.

(±) Clopidogrel hydrogen sulfate (Iscover) , an antiplatelet agent pharmacologically and structurally analogous to ticlopidine, is used to inhibit blood clots in various conditions such as cerebrovascular disease, peripheral vascular disease, and coronary artery disease.

Tea polyphenol, also called green tea extract, are a mixture of chemical compounds, such as flavanoids and tannins, found naturally in tea. Polyphenols are powerful antioxidants, which can reduce the risk of developing coronary artery disease and a number

Indecainide (Ricainid) is a novel antiarrhythmic compound that is carcinogenic and can be used to study chronic stable ventricular arrhythmias secondary to coronary artery disease or cardiomyopathy.

Granotapide is a microsomal triglyceride transfer protein (MTP) inhibitor that treats and rather prevents atherosclerosis, coronary artery disease, metabolic syndrome, obesity, diabetes mellitus, prediabetes mellitus, and hypertension.

FPL 55712 is a leukotriene receptor and SRS-A antagonist that inhibits bronchoconstriction and can be used in studies of asthma and coronary artery thrombosis.

Probucol is an anti-hyperlipidemic drug initially developed in the treatment of coronary artery disease by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.

(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide is an Apelin receptor agonist with an EC50 for Apelin receptors of 0.012 µM.(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5- methylpyrimidin-2-yl)butane-2-sulfonamide is used in the treatment of heart failure, atherosclerosis, obesity, diabetes mellitus, amyotrophic lateral sclerosis, coronary artery disease, hypertension, stroke and myocardial infarction.

TGX-115 is a cell-permeable and potent inhibitor of the PI 3-K isoform p110β/p110δ (IC50 values of 0.13 μM for p110β and 0.63 μM for p110δ), an enzyme that regulates platelet adhesion and inhibits phosphoinositide (PI) 3-kinase, and can be used to treat coronary artery occlusion, stroke, acute coronary artery It can be used to treat cardiovascular diseases such as coronary occlusion, stroke, acute coronary syndrome, acute myocardial infarction, restenosis, atherosclerosis and unstable angina.

Vicagrel is an effective, orally active antiplatelet compound that enhances the inhibitory effect of aspirin on platelet aggregation and thrombosis in rodents by irreversibly inhibiting P2Y12 receptors and reducing metabolic inactivation. Viagrel can be used to treat blood clots in coronary artery disease, peripheral vascular disease and cerebrovascular disease.

Atopaxar (E5555), a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.

BQ-788 is a selective and potent ETB receptor antagonist with potential hypertensive activity.BQ-788 inhibits ET-1 binding to ETB receptors and inhibits exogenous ET-1-induced elevation of coronary artery perfusion pressure.

Arbutamine (GP 21213) is a novel potent non-selective beta-adrenoceptor agonist with alpha-1-sympathomimetic activity.Arbutamine promotes cardiac stress and increases heart rate, cardiac contractility.Arbutamine can be used to study cardiac stress and coronary artery disease

Gue1654 is a selective OXE-R inhibitor that attenuates coronary artery ligation-induced ischemic myocardial injury and cardiomyocyte oxygen glucose deprivation-induced injury in mice through activation of BCAT1.Gue1654 inhibits OXE-R-inhibited protein kinase C-ε (PKC-ε) nuclear factor κB (NF-κB) signaling and apoptosis in cardiomyocytes. Gue1654 can be used to study cardiovascular disease.

Atopaxar, a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.

Barnidipine hydrochloride (YM-09730-5 hydrochloride) is a dihydropyridine calcium channel blocker that has an IC50 value of 0.35 nM in potassium-induced tonic contraction of pig coronary artery

Apabetalone (RVX000222) , an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.

Sulfaphenazole (Plisulfan) is an inhibitor of CYP2C9 (Ki: 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki: 63/29 μM for CYP2C8/CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19). At 10 μM, sulfaphenazole has been shown to inhibit endothelium-derived hyperpolarizing factor synthase, a CYP450 isozyme in the porcine coronary artery homologous to CYP2C8/9 that generates reactive oxygen species in coronary endothelial cells and modulates vascular tone and homeostasis.

Succinobucol (Probucol monosuccinate) is a novel phenolic antioxidant small molecule with anti-oxidant and anti-inflammatory properties. It designed to treat atherosclerosis of the blood vessels of the heart or coronary artery disease.

Atuliflapon (AZD5718) is a novel 5-Lipoxygenase Activating Protein(FLAP) inhibitor for Treatment of Coronary Artery Disease.

Perindopril (S-9490) is a long-acting ACE inhibitor effective for 24 hours, primarily utilized in the management of high blood pressure, heart failure, or stable coronary artery disease. Available as perindopril arginine (with trade names such as Coversyl and Coversum) or perindopril erbumine (known as Aceon), both formulations are regarded therapeutically equivalent, according to the Australian Government's Pharmaceutical Benefits Scheme—meaning they can be interchanged without clinical effect differences, though their dosing may vary due to distinct molecular weights. Notably, perindopril ranks among the most frequently prescribed ACE inhibitors, thanks to its extensive evidence base supporting its use in patients with hypertension, type 2 diabetes, coronary heart disease, and chronic heart failure. This review highlights perindopril's organoprotective benefits that extend beyond its capacity to lower blood pressure.

7-Ketocholesterol is a metabolite of Cholesterol

S(-)-Bisoprolol fumarate, the S(-)-enantiomer of Bisoprolol fumarate, is a potent, selective, and orally active β1-adrenergic receptor blocker with minimal activity on β2-receptors. It holds potential for research in hypertension, coronary artery disease, and stable ventricular dysfunction [1] [2].

[Lys4] Sarafotoxin S6c, an analogue of sarafotoxin, serves as a potent, partial agonist of the endothelin receptor, inducing contraction in pig coronary artery with an effective concentration (EC 50) of 1.5 nM [1].

Mitiperstat is a potent myeloperoxidase (MPO) inhibitor that is effective in preventing cardiovascular diseases such as heart failure and coronary artery disease.

Fostedil is a calcium channel antagonist. KB-944 increased regional segment function in normal and ischemic regions and maintained distal coronary artery perfusion pressure, coronary flow and transmural regional myocardial blood flow during partial corona

Pyrromecaine is a local anesthetic used for surface anesthesia. Pyromecaine has a wide spectrum of antiarrhythmic action, exerts a favorable effect on the contractility of the left ventricle, and on the myocardial blood flow following the ligation of the

(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage of the area at risk in a canine model of ischemia-reperfusion injury induced by left anterior descending coronary artery (LAD) occlusion when administered at a dose of 0.128 mg/kg prior to occlusion or reperfusion.[5] Reference：[1]. Chacos, N., Falck, J.R., Wixtrom, C., et al. Novel epoxides formed during the liver cytochrome P-450 oxidation of arachidonic acid. Biochem. Biophys. Res. Commun. 104(3), 916-922 (1982).[2]. Oliw, E.H., Guengerich, F.P., and Oates, J.A. Oxygenation of arachidonic acid by hepatic monooxygenases. Isolation and metabolism of four epoxide intermediates. J. Biol. Chem. 257(7), 3771-3781 (1982).[3]. Jiang, J.-X., Zhang, S.-J., Xiong, Y.-K., et al. EETs attenuate ox-LDL-induced LTB4 production and activity by inhibiting p38 MAPK phosphorylation and 5-LO/BLT1 receptor expression in rat pulmonary arterial endothelial cells. PLoS One 10(6), e0128278 (2015).[4]. Oltman, C.L., Weintraub, N.L., VanRollins, M., et al. Epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids are potent vasodilators in the canine coronary microcirculation. Circ. Res. 83(9), 932-939 (1998).[5]. Nithipatikom, K., Moore, J.M., Isbell, M.A., et al. Epoxyeicosatrienoic acids in cardioprotection: Ischemic versus reperfusion injury. Am. J. Physiol. Heart Circ. Physiol. 291(2), H537-H542 (2006).

1-Hydroxy-2,3,4,7-tetramethoxyxanthone, with an EC50 value of 6.6±1.4 µM, has vasodilatory action in coronary arteries pre-contracted with 1 µM 5-hydroxytryptamine (5-HT) and can effectively inhibit osteoclast differentiation in a co-culture system with mouse osteoblastic calvarial cells and bone marrow cells.

Batifiban, a glycoprotein IIb/IIIa antagonist, is used potentially for the treatment of coronary artery disease.

Endothelin receptor agonist (EC50 values are 7.5 and > 150 nM for contraction of pig coronary artery and guinea pig aorta respectively). Nociceptive in vivo.

Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).

5(6)-DiHET is a racemic compound synthesized through the action of epoxide hydrolases on 5(6)-EET, encompassing both enantiomeric forms. It serves as a quantitative marker for 5(6)-EET, facilitating its measurement by utilizing the compound's conversion to 5(6)-δ-lactone in solution. Additionally, 5(6)-DiHET activates large-conductance calcium-activated potassium (KCa1.1/BK) channels in rat small coronary artery smooth muscle cells, supporting its biological significance in vascular regulation. It also acts as a substrate for sheep seminal vesicle COX, leading to the in vitro production of 5,6-dihydroxy prostaglandin E1 and F1α metabolites. Notably, its levels diminish in the plasma of rats subjected to a high-fat diet, indicating a potential role in the pathophysiology of hyperlipidemia.

Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery (KDs = 0.26 and 0.11 nM, respectively), eliciting endothelium-independent vasoconstriction.3NMU-25 also suppresses glucose-stimulated insulin secretion in human islets, and this effect is lost in NMU R165W mutants, resulting in early-onset obesity.4 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBritish Journal of Pharmacology15887-103(2009) 2.Greenwood, H.C., Bloom, S.R., and Murphy, K.G.Peptides and their potential role in the treatment of diabetes and obesityRev.Diabet.Stud.8(3)355-368(2011) 3.Mitchell, J.D., Maguire, J.J., Kuc, R.E., et al.Expression and vasoconstrictor function of anorexigenic peptides neuromedin U-25 and S in the human cardiovascular systemCardiovascular Research81353-361(2009) 4.Alfa, R.W., Park, S., Skelly, K.R., et al.Suppression of insulin production and secretion by a decretin hormoneCell Metabolism21(2)323-333(2015)

Quazinone is a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilating properties. It induces relaxation of precontracted isolated human cavernous smooth muscle (IC50 = 4.2 μM), increases myocardial contractile force in anesthetized open-chest dogs in a dose-dependent manner (10-300 μg kg), decreases systolic and diastolic blood pressure, and inhibits DNA synthesis induced by the PDGF isoform PDGF-BB in bovine coronary artery smooth muscle cells in a concentration-dependent manner.

Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 = 4.4 µM). It decreases mean blood pressure, coronary resistance, and heart rate, as well as increases coronary sinus outflow, in dogs when administered intravenously at a dose of 1 mg/kg. Nicorandil increases survival and decreases infarct size in a rabbit model of myocardial ischemia-reperfusion injury induced by left coronary artery occlusion. Formulations containing nicorandil have been used in the treatment of angina pectoris.

PCSK9-IN-19 (Compound 1), a PCSK9 inhibitor, is utilized in researching the treatment of high LDL-cholesterol levels and the prevention of coronary artery disease [1].

Sarafotoxin S6a TFA, an analogue of sarafotoxin, functions as an endothelin receptor agonist with an ET_A/ET_B selectivity profile akin to Endothelin-3. It demonstrates an EC_50 of 7.5 nM in stimulating the pig coronary artery [1].

Streptokinase is a bacterial protein that acts as a plasminogen activator, commonly employed in the investigation of blood-clotting disorders. Its application extends to enhancing reperfusion blood flow after coronary artery occlusion.

Ciprostene (free base) is a synthetic, chemically stable analog of prostacyclin (PGI2). In animal models, administration of ciprostene resulted in dose-dependent hypotension, tachycardia, and inhibition of ex vivo ADP-induced platelet aggregation. Ciprostene was evaluated in clinical trials in patients with peripheral vascular disease. It was found to reduce restenosis in patients with coronary artery disease undergoing therapeutic percutaneous transluminal coronary angioplasty.

PKCd (8-17) is a bioactive peptide originating from the V1 domain of protein kinase C (PKC)d. It impedes phorbol 12-myristate 13-acetate (PMA)-stimulated PKCd translocation and activation, which mitigates ischemic injury in cardiac and cerebral cells, promotes fibroblast proliferation, and suppresses graft coronary artery disease in [mouse models].

TC 14012, a peptidomimetic compound, acts as both an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 2.9 nM) and as an agonist for CXCR7, effectively recruiting β-arrestin in HEK293T cells that express CXCR7 (EC50 = 350 nM). Moreover, it demonstrates significant antiviral activity by reducing the cytopathic effects of HIV in MT-4 cells with an EC50 value of 0.4 nM and inhibiting HIV entry in vitro through a CXCR4-dependent pathway (IC50 = 19.3 nM). Additionally, TC 14012 suppresses chemokine (C-X-C motif) ligand 12 (CXCL12)-induced migration in MDA-MB-231 breast cancer and human umbilical vein endothelial cells (HUVECs) within the 10 to 1,000 nM concentration range. In a mouse model, administration of TC 14012 at 10 mg/kg significantly reduced infarct size following acute myocardial infarction induced by ligation of the left anterior descending (LAD) coronary artery.

Dilmapimod tosylate is a potent p38 mitogen-activated protein kinase (MAPK) inhibitor. It was investigated for its anti-inflammatory effect in non-head injury trauma patients at risk for developing acute respiratory distress syndrome. IL-1β was identified as a gene regulated by dilmapimod that could influence c-reactive protein levels. Dilmapimod had been in phase III clinical trials by GlaxoSmithKline for the treatment of rheumatoid arthritis, neuropathic pain, coronary artery disease (CAD) and chronic obstructive pulmonary disease (COPD).

AZD5718 is a potent and selective FLAP inhibitor (IC50 = 2.0 nM) for Treatment of Coronary Artery Disease. AZD5718 demonstrated a dose dependent and greater than 90% suppression of leukotriene production over 24 h. Preclinical toxicology studies in rat and dog did not show any serious adverse events of clinical significance. Currently, AZD5718 is evaluated in a phase 2a study for treatment of coronary artery disease.

2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endothelial cells (HCAECs) when used at a concentration of 50 μM and increases production of P-selectin, von Willebrand factor, and angiopoietin-2 in HCAECs, as well as neutrophil and platelet adherence, when used at a concentration of 10 μM. 2-chloro Palmitic acid (10-50 μM) also induces apoptosis in THP-1 cells and primary human monocytes and increases caspase-3 activity in THP-1 cells.

Nipradolol (KT-210; K-351), an alpha-1-adrenergic receptor antagonist, effectively inhibits the elevation of intraocular pressure (IOP) induced by Phenylephrine in an albino rabbit model, suppresses noradrenaline (NA)-induced muscle contractions, and demonstrates vasodilatory effects on the coronary artery in dogs [1] [2].

1. Praeruptorin C and E can relax swine coronary artery and decrease contractility in guinea-pig left atria, these effects are similar in many respects to those displayed by drugs that have calcium entry blocking activity. 2. Praeruptorin D and E can prot