Manidipine is a calcium channel blocker that is used clinically as an antihypertensive. Target: Calcium ChannelManidipine is a dihydropyridine calcium antagonist, which causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. Manidipine was well tolerated in clinical trials, with most adverse effects related to vasodilation [1]. Manidipine is a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. manidipine represents a first-line treatment option for patients with essential mild-to-moderate hypertension [2]. Manidipine has neutral effects on glucose and lipid metabolism and is generally well tolerated. Manidipine thus represents a first-line option for lowering BP in patients with mild-to-moderate hypertension [3].
Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
Propranolol is a noncardioselective β-blocker. Propranolol has membrane-stabilizing properties, but does not own intrinsic sympathomimetic activity. Propranolol hydrochloride is used to control hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[1].
Tonlamarsen is a angiotensinogen synthesis reducer, with antihypertensive activity[1].
Docosatrienoic acid is a rare ω-3 fatty acid; inhibits LTB4 binding to pig neutrophil membranes with an Ki of 5 μM.
Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant[1] and anti-inflammatory activities[3]. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling[2]. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation[3].
L 655240 is thromboxane antagonist. L 655240 attenuates early ischemia- and reperfusion-induced arrhythmias in a canine model of coronary artery occlusion. L 655240 also involves in cancer and autoimmune disorders[1].
Moexipril is an orally active and potent angiotensin-converting enzyme (ACE) inhibitor. Moexipril can readily penetrate lipid membranes and thus target plasma and tissue ACE. Moexipril may improve endothelial dysfunction and exert neuroprotective effects. Moexipril can used for cardiovascular disease research[1][2].
Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
AZ12799734 (AZ-12799734) is a pan BMP/TGFβ inhibitor that potently inhibits ligand activated SMAD3/4 transcription with IC50 of 47 nM, inhibits receptor-mediated phosphorylation of SMAD1 by ALK1, BMPR1A and BMPR1B and phosphorylation of SMAD2 by ALK4, TGFBR1 and ALK7; inhibits TGFβ-induced migration in HaCaT cells.
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis[1][2].
GSK 1562590 hydrochloride is a high affinity and selective antagonist of urotensin-II receptor (UT), with pKis of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native UT[1].
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker[1][2]. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia[3].
Pentosan Polysulfate is a semi-synthetic drug used to treat various medical conditions including thrombi and interstitial cystitis.
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo[1].
Acetyl podocarpic acid anhydride is a potent, semisynthetic liver X receptor(LXR) agonist derived from extracts of the mayapple. Acetyl podocarpic acid anhydride has the potential to be useful for the prevention and treatment of atherosclerosis, especially in the context of low HDL levels[1].
I942 is a first in class, non-cyclic nucleotide agonist of EPAC1.
Ticlopidine hydrochloride is an adenosine diphosphate (ADP) receptor inhibitor against platelet aggregation with IC50 of ~2 μM.Target: Adenosine diphosphate (ADP)Ticlopidine (trade name Ticlid) is an antiplatelet drug in the thienopyridine family. Ticlopidine hydrochloride inhibits platelet aggregation with IC50 of ~2 μM in men. Like clopidogrel, it is an adenosine diphosphate (ADP) receptor inhibitor. It is used in patients in whom aspirin is not tolerated, or in whom dual antiplatelet therapy is desirable. Because it has been reported to increase the risk of thrombotic thrombocytopenic purpura (TTP) and neutropenia, its use has largely been supplanted by the newer drug, clopidogrel, which is felt to have a much lower hematologic risk. Its niche role as an alternative in those patients who do not tolerate Clopidogrel has now been superdeded by Ticagrelor and Prasugrel. The usual dose is 250 mg twice daily by the oral route.Ticlopidine hydrochloride, when orally administered to rats, results in activation of basal and prostaglandin E1 (PGE1)-stimulated adenylate cylase activity through increase in affinity of the cyclase in platelet membrane to PGE1, although it failed to affect adenosine- or sodium fluoride-stimulated activity of the enzyme.
Tirofiban-d9 is deuterium labeled Tirofiban.
Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is a blood pressure lowering peptide containing 4 amino acids. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is an angiotensin-converting Enzyme (ACE) inhibitor. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine can be used in research of high blood pressure[1].
Loureirin A is a flavonoid extracted from Dragon's Blood, can inhibit Akt phosphorylation, and has antiplatelet activity.
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research[1][2].
(Rac)-Nebivolol-d4 ((Rac)-R 065824-d4) is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM[1][2].
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation[1][2][3].
DDO-02005 (free base) is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 (free base) has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine[1].
DMNQ is a redox cycling agent that generates both superoxide and hydrogen peroxide intracellularly in a concentration dependent manner. DMNQ increases ROS generation[1].
Temocapril-d5 is the deuterium labeled Temocapril. Temocapril is an angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases[1][2].
Docosahexaenoyl glycine is a PUFA analogue. Docosahexaenoyl glycine has activating effects on IKs?channels?and restore the function of IKs?channels with LQT1 mutation[1].
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways[1].