R-138727, the thiol-containing active metabolite of Prasugrel, is an irreversible platelet P2Y12 receptor inhibitor. R-138727 inhibits ADP-induced platelet aggregation[1].
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
Apixaban 13CD3 (BMS-562247-01 13CD3) is a deuterium labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
Fibronectin, a glycoprotein (~500 kDa) present in blood as well as in cells, is a biomarker of tissue injury. Fibronectin binds to membrane-spanning receptor proteins called integrins. Fibronectin also binds to other extracellular matrix proteins such as collagen, fibrin, and heparan sulfate proteoglycans[1].
Ezetimibe hydroxy glucuronide (SCH 488128) is a trace metabolite detected in dog and human plasma samples after oral administration of Ezetimibe (HY-17376)[1].
Tormentic acid, a triterpene isolated from Rosa rugosa, exerts anti-inflammatory, antihyperlipidemic, and anti-atherogenic properties[1][2].
Viscumneoside III, a dihydroflavone O-glycoside, is a potent tyrosinase inhibitor with an IC50 of 0.5 mM. Viscumneoside III has anti-angina pectoris[1].
Betaxolol is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.Target: Beta1 Adrenergic ReceptorBetaxolol is a cardioselective beta-adrenergic receptor blocking agent. Betaxolol (5 mg/kg via i.p. injection) was administered at 24 and then 44 h following the final chronic cocaine administration. Animals treated with betaxolol during cocaine withdrawal exhibited a significant attenuation of anxiety-like behavior characterized by increased time spent in the open arms and increased entries into the open arms compared to animals treated with only saline during cocaine withdrawal. Betaxolol did not produce anxiolytic-like effects in control animals treated chronically with saline [1]. Betaxolol produces less systemic beta 2- and possibly beta 1-adrenergic receptor blockade than either timolol or levobunolol. Betaxolol may be relatively safer to use in patients with reactive airway disease than either timolol or levobunolol [2].
HAMI3379 (HAMI-3379) is a potent and selective antagonist of cysteinyl leukotriene 2 (CysLT(2)) receptor, inhibits LTD4- and LTC4-induced intracellular calcium mobilization withIC50 of 3.8 nM and 4.4 nM respectively; exhibits very low potency on a recombinant CysLT(1) receptors (IC50>10 uM), does not exhibit any agonistic activity on both CysLT receptors; concentration-dependently inhibits and reverses the LTC(4)-induced perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts, protects against acute brain injury after focal cerebral ischemia in rats.
D-pinitol (3-O-Methyl-D-chiro-inositol) is a natural compound presented in several plants, like Pinaceae and Leguminosae plants. D-pinitol exerts hypoglycemic activity and protective effects in the cardiovascular system[1][2].
Neuropeptide FF (NPFF), an octapeptide belonging to the RF-amide family of peptides, interacts with two distinct G-protein-coupled receptors, NPFF(1) and NPFF(2) and has wide variety of physiological functions in the brain including central cardiovascular and neuroendocrine regulation[1][2].
Doxazosin(UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.Target: Adrenergic ReceptorDoxazosin is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms [1]. doxazosin may have a direct inhibitory effect on cholesterol synthesis independent of the LDL receptor. The inhibition of cholesterol synthesis by doxazosin may cause cells to compensate by upregulating the LDL receptor, thereby increasing the importation of lipoprotein cholesterol and reducing LDL cholesterol in the medium [2]. Doxazosin monotherapy was effective in eight of 12 patients (66.7%), and combined therapy with a beta-blocker was effective in 11 of 12 patients (91.7%). The mean pulse rate remained constant throughout therapy. Adverse reactions were minor and transient and occurred in only three patients. Urinary and plasma catecholamine levels tended to decrease or remained unchanged during doxazosin therapy [3].Clinical indications: Hypertension; Prostate hyperplasiaFDA Approved Date: February 22, 2005Toxicity: Symptoms of overdose include hypotension
Activated Protein C (390-404), human is a peptide of the activated protein C (a vitamin K-dependent serine protease), potently inhibits APC anticoagulant activity[1].
Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability[1].
Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors[1]. Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins [2]. Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS)[3].
Arecaidine but-2-ynyl ester tosylate is a potent muscarinic agonist that shows 4.6-fold that is selectivity for mAChR M2 in the atrium versus those in the ileum.
Osajin is the major bioactive isoflavone present in the fruit of Maclura pomifera with antitumor, antioxidant and anti-inflammatory activities.
Danegaptide (GAP-134), a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability.
TRAP-7 is a thrombin receptor (PAR) activating peptide. TRAP-7 stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be used in cardiovascular disease research[1].
GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3[1][2].
Benidipine hydrochloride is a dihydropyridine calcium channel blocker for the treatment of high blood pressure (hypertension).
EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.
Tasosartan is a long-acting angiotensin II (AngII) receptor antagonist.
JB002 is a myosin II inhibitor, with an IC50 of ≤10 μM. JB002 can be used for the research of muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy[1].
Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect[1][3].
OR-1855, an active metabolite of Levosimendan, has effect on human myometrial contractility. Levosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure[1][2].
Flecainide(Tambocor) is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.IC50 Value:Target: Nav1.5 channelFlecainide is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia. Flecainide works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.in vitro: Under the current-clamp condition, flecainide (1-100 microM) prolonged the action potential duration at both the early and the late phases of repolarization in a concentration-dependent manner without affecting the resting membrane potential [1]. At a holding potential (HP) of -120 mV, flecainide use-dependently blocked WT and G1306E I(Na) equally but was more potent on R1448C channels. For WT, the extent of block depended on a holding voltage more negative than the activation threshold, being greater at -90 mV as compared to -120 and -180 mV [2].in vivo: Flecainide (80-130 mg/m(2) orally) resulted in termination of the tachycardia in all 8 patients. Acute pharmacological termination of arrhythmia occurred with oral flecainide loading in 1 and temporarily with intravenous esmolol loading in 1 patient. Adjuvant therapy in form of propranolol was used in 5 and digoxin in 2 [3].Clinical trial: To Evaluate the Impact of Oral Flecainide on Quality of Life in Patients With Paroxysmal Atrial Fibrillation . Phase4
QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.
HS94 (DAPK3 inhibitor HS94) is a selective DAPK3 inhibitor with Ki of 126 nM, >20-fold selectivity over Pim kinases.
Ouabain Octahydrate is an inhibitor of Na+/K+-ATPase, used for the treatment of congestive heart failure.