GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.
BAY 60-2770 is an NO-independent activator of sGC (soluble guanylyl cyclase) with EC50 of 5.4 nM; demonstrates vasodilator activity in the pulmonary and systemic vascular beds that is enhanced by ODQ and NOS inhibition.
VTP-27999 2,2,2-trifluoroacetate is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.Ic50 value:Target: Renin
2'-O-Methyladenosine, a methylated adenine residue is found in urine of normals as well as in urine of adenosine deaminase (ADA) deficient patients. 2'-O-Methyladenosine exhibits unique hypotensive activities [1][2].
Carbazochrome is a capillary stabiliser and used for the research of haemorrhage. Carbazochrome is an antihemorrhagic agent[1].
Ermanin is a flavonoid isolated from Tanacetum microphyllum. Ermanin potently inhibits iNOS, COX-2 activities, and inhibits platelet aggregation. Ermanin has anti-inflammatory, anti-tuberculous and anti-viral/bacterial properties[1][2].
Iganidipine is a Ca2+ antagonist.
Medroxalol (RMI81968) is an orally active adrenergic receptor antagonist, blocks α- and β-adrenergic receptors. Medroxalol shows antihypertensive and vasodilating effects[1].
L-Homocystine is the oxidized member of the L-homocysteine. Homocysteine is a pro-thrombotic factor, vasodilation impairing agent, pro-inflammatory factor and endoplasmatic reticulum-stress inducer used to study cardiovascular disease mechanisms.
Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].
PSB069 bearing a p-chlorophenylamino residue is a potent, well-tolerated and nonselective NTPDases1, 2, 3 inhibitor(Ki=16~18 μM)[1].
GLX481304 is a specific inhibitor of Nox-2 and -4, with IC50s of 1.25 μM. GLX481304 suppresses ROS production in isolated mouse cardiomyocytes and improves cardiomyocyte contractility. GLX481304 can be used for research of ischemic injury to the heart[1].
(+)-BAY-1251152 is a CDK9 inhibitor extracted from patent WO 2014076091 A1, example 1.
Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research[1][2].
CCG-273463 is a potent, selective and covalent GRK5 inhibitor with an IC50 value of 9 nM. CCG-273463 can be used in the research of heart failure, hypertrophic cardiomyopathy, and cancer[1].
Theodrenaline is a cardiac stimulant, also acts as an anti-hypotensive agent together with cafedrine.
Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities[1][2].
Cloricromen (Cloricromene) is a platelet aggregation inhibitor. Cloricromen can inhibit platelet aggregation in man and in experimental thrombosis[1].
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease[1][2].
Quisovalimab (AVTX-002; AEVI 002; SAR 252067) is a human monoclonal antibody against LIGHT, a tumor necrosis factor (TNF)-related cytokine (TNFSF14) that plays an important role in acute respiratory distress syndrome (ARDS) and cytokine release syndrome (CRS) COVID-19. Quisovalimab can be used in COVID-19 acute respiratory distress syndrome and other studies[1].
Prenalterol is a selective β1-adrenergic receptor agonist. Prenalterol has no effect on gut smooth muscle contractile activity. Prenalterol can be used for researching cardiovascular disease[1].
Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
Etofylline is a vasodilator.
trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations[1].
(+)-Sotalol ((S)-Sotalol) is the S-isomer of Sotalol (HY-103196). Sotalol is an orally active, non-selective β-adrenergic receptor blocker. (+)-Sotalol is an antiarrhythmic agent. (+)-Sotalol can prolong action potential duration in isolated cardiac muscle[1][2][3].
JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking[1][2].
Kurarinol is a flavanone found in the root of Sophora flavescens. Kurarinol is a competitive tyrosinase inhibitor, with IC50 of 0.1 μM for mushroom tyrosinase[1].
N6-(4-Hydroxybenzyl)adenosine is a inhibitor of platelet aggregation induced in vitro by collagen and their activity range was demonstrated (IC50: 6.77-141 μM). IC50 value: 6.77-141 μMTarget: P2Y12receptorAnti-aggregation activity of N6-(4-Hydroxybenzyl)adenosine could involve an interaction with the P2Y12receptor binding site.
trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[1].