Guanoxabenz is an α2 adrenergic receptor agonist.
Modecainide is a major metabolite of Encainide, which is an antiarrhythmic agent.
GPRP acetate is fibrinogen-related peptide, which inhibits the interaction of fibrinogen with the platelet membrane glycoprotein IIb/IIIa complex (GPIIb/IIIa). Sequence: Gly-Pro-Arg-Pro.
(D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V1aR), with a Ki of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R[1].
Bopindolol is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol is a prodrug of pindolol and can be used for essential and renovascular hypertension research[1][2].
o-Hydroxybenzylamine (2-HOBA) a selective dicarbonyl scavenger, is an antioxidant and scavanger of free radicals and isolevuglandins (IsoLGs). o-Hydroxybenzylamine can be used in the research of inflammation and cardiovascular disease, such as atherosclerosis, early recurrence of atrial fibrillation (AF) and arrhythmias[1][2].
A potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist with IC50 of 45 nM, with no activity on αVβ3 receptors.
Ranolazine is an antianginal medication.Target: Sodium ChannelRanolazine is believed to have its effects via altering the transcellular late sodium current. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the intracellular sodium level [1]. Thus, ranolazine indirectly prevents the calcium overload that causes cardiac ischemia in rats [2]. The effects of ranolazine on the NaV 1.7 and NaV 1.8 sodium channels also make it potentially useful in the treatment of neuropathic pain. Ranolazine produced dose-dependant analgesia on mechanical allodynia induced by CFA injection, but had no effect on thermal hyperalgesia [3, 4].
γ1-MSH is a melanocortin MC3 receptor agonist, with a Ki of 34 nM for the rat MC3 receptor. γ1-MSH displays ~40-fold selectivity over MC4 (Ki=1318 nM)[1].
Gypenoside XIII is belonging to the gypenosides. Gypenosides, extracted from Gynostemma pentaphyllum, have various pharmacological properties and protect against cardiovascular diseases, especially atherosclerosis[1].
OPC-163493 is an orally active liver-targeted mitochondrial uncoupling agent. OPC-163493 reduces Δψ and mitochondrial ROS production. OPC-163493 has antidiabetic and cardiovascular beneficial effects. OPC-163493 lowers blood pressure, extends survival, and improves renal function in the rat model of stroke/hypertension[1].
Metoprolol is a cardioselective β1-adrenergic blocking agent.Target: β1- adrenergic ReceptorPatients took 50 mg metoprolol twice daily with weekly titration to response or 200 mg twice daily. beta(1)-adrenergic receptor polymorphisms are important determinants of antihypertensive response to metoprolol. In the future, codon 49 and 389 genotypes or beta(1)-adrenergic receptor haplotypes might be used to predict the diastolic blood pressure response to metoprolol in patients with hypertension [1]. Patients were studied at baseline and after each dose titration of metoprolol succinate (at 25, 50, 100, and 200 mg once/day) and immediate-release carvedilol (at 3.125, 6.25, 12.5, and 25 mg twice/day). As assessed by glucose AUC, there was no significant difference in the degree of beta(2)-blockade between metoprolol 200 mg and carvedilol 25 mg. In contrast to these data, the degree of beta(2)-blockade as assessed by potassium AUC was greater for carvedilol compared with metoprolol across all doses [2].
Warfarin(WARF42) is an anticoagulant drug normally used to prevent blood clot formation as well as migration.Target: OthersWarfarin is an anticoagulant normally used in the prevention of thrombosis and thromboembolism, the formation of blood clots in the blood vessels and their migration elsewhere in the body respectively. Warfarin and related 4-hydroxycoumarin-containing molecules decrease blood coagulation by inhibiting vitamin K epoxide reductase, an enzyme that recycles oxidized vitamin K1 to its reduced form after it has participated in the carboxylation of several blood coagulation proteins, mainly prothrombin and factor VII. Despite being labeled a vitamin K antagonist, warfarin does not antagonize the action of vitamin K1, but rather antagonizes vitamin K1 recycling, depleting active vitamin K1 [1, 2].
Dofetilide(Tikosyn) is a class III antiarrhythmic agent.Target: Potassium ChannelIn patients with congestive heart failure and reduced left ventricular function, dofetilide was effective in converting atrial fibrillation, preventing its recurrence, and reducing the risk of hospitalization for worsening heart failure. Dofetilide had no effect on mortality [1]. dofetilide preferentially blocks open (or activated) channels and that the fast inactivation may competitively slow the binding kinetics. Dofetilide acts as a slow-onset/slow-offset open channel blocker of this current at nanomolar concentrations [2].
Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) inhibitor with an IC50 value of 33 nM, and shows robust reduction of intestinal serotonin (5-HT) levels in mice. Rodatristat also shows potent inhibition of TPH2 (IC50 of 7 nM)[1].
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes[1]. Enniatin B1 crosss the blood-brain barrier[2]. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation[3].
Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke preventionIC50 Value:Target: factor XaEdoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention in patients with atrial fibrillation, an elderly population that frequently receives aspirin (ASA) and/or nonsteroidal anti-inflammatory drugs for concurrent illnesses[1].in vitro: Edoxaban PK was not affected by concomitant low-dose ASA or naproxen, but high-dose ASA increased systemic exposure of edoxaban by approximately 30%. The effects of edoxaban on prothrombin time, activated partial thromboplastin time, international normalized ratio, anti-FXa, and intrinsic FXa activity were not influenced by administration with ASA or naproxen. Inhibition of platelet aggregation by high-dose ASA, low-dose ASA, or naproxen was not affected by edoxaban[1].in vivo: Forty-eight subjects, aged 18 to 45 years, received either edoxaban 60 mg once daily × 7 days (n = 24) or digoxin 0.25 mg twice daily × 2 days and once daily × 5 days (n = 24) and then concomitantly for 7 days. Serial blood and urine samples were collected for digoxin and edoxaban concentrations on days 7 and 14. Serial coagulation assays were measured for edoxaban on days 7 and 14. Edoxaban PK parameters demonstrated mild increases in area under the curve and peak concentrations of 9.5% and 15.6%, respectively[2],Clinical trial: Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans was reported[3].
Phosphatidylcholine is the main phospholipid component in eukaryotic biofilms. Phosphatidylcholine exists in commensal or pathogenic bacteria associated with eukaryotes in prokaryotes. Phosphorylcholine exhibits a surprising range of immunomodulatory properties[1].
Cy5.5 (Sulfo-Cyanine5.5) is a near-infrared fluorescent dye (Ex=673 nm, Em=707 nm) used to label biological molecules, such as peptides, proteins, and oligonucleotides[1].
mEH-IN-1 (Compound 62) is a potent microsomal epoxide hydrolase (mEH) inhibitor with the IC50 of 2.2 nM. The mEH is a mammalian α/β-fold hydrolase enzyme, expressed in almost all tissues, hydrolyzes a wide range of epoxide containing molecules. The mEH is mainly localized in the endoplasmic reticulum (ER) of eukaryotic cells. mEH-IN-1 can be used for the research of preeclampsia, hypercholanemia and cancer[1].
EMD 66684 is an antagonist of Angiotensin II Type 1 (AT1) receptor. EMD 66684 shows potent binding affinities for the AT1 subtype Ang II receptor with an IC50 value of 0.7 nM. EMD 66684 also serves as an antiischemic cytoprotectant [1]-[5].
Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma[1][2][3].
Terrestrosin K, a steroidal saponin from Tribulus terrestris L., has potential to treat cardiovascular and cerebrovascular diseases[1].
IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia[1][2][3].
Ganodermic acid S is an oxygenated triterpenoid, that can be isolated from the Chinese medicinal fungus Ganoderma lucidum (Fr.) Karst (Polyporaceae). Ganodermic acid S exerts a concentration dependent inhibition on the response of human gel-filtered platelets (GFP) to U-46619 (HY-108566), a thromboxane (TX) A2 mimetic[1].
Febuxostat (TEI 6720) sodium is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a Ki value of 0.6 nM. Febuxostat sodium has the potential for the research of hyperuricemia and gout[1][2][3].
Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.
H-Ile-Pro-Pro-OH, a milk-derived peptide[1], inhibits angiotensin-converting enzyme (ACE)[1] with an IC50 of 5 μM[2]. Antihypertensive tripeptides[1].
ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.
Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Cyanotis arachnoides C.B.Clarke which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP[1].Crustecdysone exhibits regulatory or protective roles in the cardiovascular system[2].