Leucylarginylproline is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 0.27μM.
Lauric acid-13C-1 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively[1].
Cyclocurcumin is a potent p38α inhibitor. Cyclocurcumin shows antirheumatic, antivasoconstrictive and antioxidant activities[1][2][3].
Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist[1].
Asundexian (BAY 2433334) is an orally active coagulation factor Xia (FXIa) inhibitor. Asundexian binds directly, potently, and reversibly to the active site of FXIa and thereby inhibits its activity. Asundexian inhibits human FXIa in buffer with an IC50 of 1 nM[1].
Hirudin (54-65) is a fragment of the 65 residue protein of Hirudin with anticoagulant effects[1].
Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.
Methyclothiazide is an orally active antihypertensive agent and a diuretic agent. Methyclothiazide leads to a reduction of the vascular response to the action of endogenous vasoconstricting stimuli, such as Norepinephrine (HY-13715). Methyclothiazide is against voltage-dependent Ca-channel (VDCC) activity in vitro[1][2][3].
Naftidrofuryl is a drug used in the management of peripheral and cerebral vascular disorders as a vasodilator, enhance cellular oxidative capacity, and may also be a 5-HT2 receptor antagonist.Target: 5-HT2 receptorNaftidrofuryl may be effective for relieving the pain of muscle cramps.[1]Naftidrofuryl oxalate is the only vasoactive drug for peripheral arterial disease (PAD) which is likely to be cost-effective.[2]Naftidrofuryl oxalate is ranked first for both maximum walking distance (MWD) and pain-free walking distance (PFWD) (probability of 0·947 and 0·987, respectively, of being the best treatment) followed by cilostazol and pentoxifylline. Naftidrofuryl oxalate is effective treatments for claudication, Naftidrofuryl oxalate is likely to be the most effective, with minimal serious adverse events.[3]
(R)-Fangchinoline (Thalrugosine), a alkaloids from genus Stephania，exhibits antimicrobial and hypotensive activity. The roots and stems of several plants from genus Stephania are all used as traditional Chinese medicine and have been used for treatment of fever, diarrhea, dyspepsia and urinary disease[1].
Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension.IC50 Value: 7.1 nM at V(H) = -40 mV [1]Target: calcium channelin vitro: Both clevidipine and nitroglycerin completely reversed U46619-induced contraction (clevidipine (50% effective concentration [EC50] = 3.88 +/- 0.84 x 10(-6) mol/L, nitroglycerin EC50 = 4.84 +/- 2.76 x 10(-8) mol/L) [2]. A decrease in temperature increased the half-life of clevidipine in blood, whereas dilution of the blood did not affect the in vitro half-life of clevidipine. The albumin concentration affected the hydrolysis rate of clevidipine in RBC suspended with saline [3].in vivo: Clevidipine is a high-clearance drug with a relatively small volume of distribution, resulting in an extremely short half-life in all species studied. The median initial half-life of the individual value (Bayesian estimates) is 12, 20, and 22 s in the rabbit, rat, and dog, respectively [4]. The extremely high clearance value and the small volume of distribution resulted in short half-lives of clevidipine, 2.2 and 16.8 min, respectively. The blood concentration and dose rate producing half the maximal effect (i.e. EC50 and ED50) were approximately 25 nM and 1.5 microg/kg/min, respectively [5].Clinical trial: CARVE: Clevidipine for Vasoreactivity Evaluation of the Pulmonary Arterial Bed. Phase 4
Azaindole 1 is a highly potent inhibitor of human ROCK-1 and ROCK-2, with IC50s of 0.6 and 1.1 nM, respectively, and also inhibits murine ROCK-2 or rat ROCK-2 with IC50s of 2.4 and 0.8 nM, respectively.
Arrhythmic-Targeting Compound 1 is used for the research of arrhythmic disease, with nitrogen-containing spirocycles.
KC 12291 hydrochloride is an orally active blocker of voltage-gated sodium channel (VGSC). KC 12291 hydrochloride reduces the amplitude of sustained Na+ current to exert antiischemic activity. KC 12291 hydrochloride has significant cardioprotective effect in vitro and in vivo[1].
CXL-1020 is a hydroxylamine-based nitroxyl (HNO) donor. CXL-1020 improves cardiac inotropy/lusitropy and Ca2+ cycling in rats with abnormal relaxation. CXL-1020 induces vasorelaxation and improves cardiac function in canine models. CXL-1020 has been used to research systolic heart failure and stable heart failure[1].
Atpenin A5 is a potent and highly specific complex II inhibitor (IC50 ~10 nM), and is an effective mKATP channel agonist and cardioprotective agent[1].
Carboxy-PTIO is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model[1][2][3].
Nanterinone (UK 61260) is a positive inotropic and arterial vasodilating agent. Nanterinone is a phosphodiesterase inhibitor[1].
Neoglycyrol is isolated from the root of Glycyrrhiza uralensis Fisch[1]. Neoglycyrol is a potential myocardial protection active compound screened from traditional patent medicine Tongmai Yangxin pill (TMYXP)[2].
Flocoumafen (WL 108366), a second-generation anticoagulant rodenticide (ARs), belongs to the family of vitamin K antagonist (VKA) molecules[1][2].
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade[1].
Prifuroline is an antiarrhythmic agent.
Urotensin II-related peptide is a human urotensin II anague. Urotensin II-related peptide has high affinity for the UT receptor[1][2].
Tie2 kinase inhibitor 2 (compound 7) is a selective Tie2 kinase inhibitor with an IC50 value of 1 μM. Tie2 kinase inhibitor 2 inhibits endothelial cell tube formation, and can be used for Tie2-mediated angiogenic disorders research[1].
Guanabenz (hydrochloride) is an oral α-2-adrenoceptor agonist, has antihypertensive effect and antiparasitic activity. Guanabenz (hydrochloride) interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz (hydrochloride) also is used for the research of high blood pressure(equivalent).
FXIa-IN-13 (example 1) is an Factor Xa inhibitor with antithrombotic activity. FXIa-IN-13 inhibits arteriovenous thrombosis in vivo and in vitro[1].
β2AR/M-receptor agonist-1 (example 131) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-1 shows potency to β2 adrenoceptor with an EC50 value of 9.2 nM. β2AR/M-receptor agonist-1 also has potency to muscarinic receptor with a Ki value of 30.2 nM. β2AR/M-receptor agonist-1 shows MABA potency with an EC50 value of 4.0 nM[1].
BPKDi is a potent bipyridyl PKD inhibitor with IC50s of 1 nM, 9 nM and 1 nM for PKD1, PKD2 and PKD3, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes[1].
A potent inhibitor of developmental angiogenesis in the zebrafish eye, and a cysteinyl leukotriene 1 and 2 receptor (CysLT1 and 2) antaognist with IC50 of 1.2 and 52 uM, respectively; demonstrates significant anti-angiogenic activity in human endothelial cell, murine aortic ring, and murine oxygen-induced retinopathy models of angiogenesis; does not directly target VEGFRs, and inhibits angiogenesis in a range of cell and tissue systems.
BI-9627 is a sodium−hydrogen exchanger isoform 1 (NHE1) inhibitor with an EC50 of 31 nM[1].