CS476 is a potent hypoglycaemic agent.
L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.
Safflor yellow A, a flavonoid extracted from Carthamus tinctorius L, is a water-soluble monomer of safflor yellow. Safflor yellow A protects rat cardiomyocytes against anoxia/reoxygenation (A/R) injury via inhibiting cellular oxidative stress and apoptosis[1].
Diltiazem malate is a potent and orally active L-type calcium chanel inhibitor. Diltiazem malate shows antihypertensive and antiarrhythmic effects. Diltiazem malate can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].
Nicomol is an orally active hypolipidemic agent that can increase the high density lipoprotein cholesterol (HDL-C) level. Nicomol inhibits the rapid rise of plasma free fatty acids[1][2].
Implitapide Racemate is the racemate of Implitapide. Implitapide is a microsomal triglyceride transfer protein (MTP) inhibitor.
[Orn5]-URP is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC50 of 7.24. [Orn5]-URP displays no agonist activity[1][2].
Bumetanide sodium, a highly potent loop diuretic, is a Na+-K+-Cl+ cotransporter (NKCC) blocker. Bumetanide sodium is a selective NKCC1 inhibitor, and also inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively[1][2].
SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research[1].
TY-52156 is a potent S1P3 receptor antagonist in a competitive manner, and the Ki value is estimated to be 110 nM for S1P3 receptor.IC50 value: 110 nM (Ki)Target: S1P3in vitro: TY-52156 shows submicromolar potency and a high degree of selectivity for S1P3 receptor. TY-52156 is both sensitive and useful as an S1P3 receptor-specific antagonist and reveal that S1P induces vasoconstriction by directly activating S1P3 receptor and through a subsequent increase in [Ca2+]i and Rho activation in vascular smooth muscle cells. TY-52156 has a selective antagonistic effect toward S1P3 receptor. [1]in vivo: TY-52156 Suppresses S1P3 Receptor-Induced Bradycardia In Vivo. the oral administration of TY-52156 inhibits S1P3 receptor-dependent bradycardia. [1]
Jujuboside B is one of the major bioactive constituents isolated from Zizyphus jujuba. Jujuboside B can inhibit platelet aggregation[1].
HUP30 is a vasodilating agent. HUP30 stimulates soluble guanylyl cyclase, activate K+ channels, and blocks extracellular Ca2+ influx[1].
TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.
Prostaglandin E1-d4 (Alprostadil-d4) is the deuterium labeled Prostaglandin E1. Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases[1][2][3].
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells[1].
NTE-122 (dihydrochloride) is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with the IC50 in liver and aorta of cholesterol-fed rabbits of 7.6nM, 4.4nM and 9.6 nM, respectively, that plays an important role in atherosclerosis[1].
Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc[1].
GNX-865 is a potent mitochondrial permeability transition pore (mPTP) inhibitor with EC50 of 105 uM (mitochondrial swelling); attenuates opening of the mPTP and limits reperfusion injury in a rabbit model of acute myocardial infarction.
VO-OHPic is a reversible, noncompetitive and selective PTEN inhibitor with an IC50 of 46 nM. VO-OHPic attenuates apoptosis, adverse cardiac remodeling, and pro-inflammatory M1 macrophages in doxorubicin-induced cardiomyopathy. VO-OHPic inhibits autophagy[1][2][3].
D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities[1][2].
BAY 73-1449 is a selective antagonist of prostacyclin IP receptor, with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure[1].
L-Lysine-d8 hydrochloride is the deuterium labeled L-Lysine hydrochloride. L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.
Dipyridamole-d20 is the deuterium labeled Dipyridamole. Dipyridamole is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells[1][2][3].
Quinate is an antiarrhythmic agent. Quinate is a potent, orally active, selective cytochrome P450db inhibitor. Quinate is also a K+ channel blocker with an IC50 of 19.9 μM. Quinate can be used for malaria research[1][2][3].
Elabela(19-32) is a potent apelin receptor (APJ) endogenous agonist with a Ki of 0.93 nM. Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart[1][2].
BW 245C is a prostanoid DP-receptor (DP1) agonist, used to treat stroke.
sEH inhibitor-6 (Compound 3g) is a soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 0.5 nM[1].
Z-Pro-prolinal (N-Benzyloxycarbonyl-L-prolyl-L-prolinal) is a specific, orally active prolyl endopeptidase (PREP) inhibitor with an IC50 of 0.4 nM for porcine PREP[1][2][3].
CB-7921220 is an adenylate cyclase inhibitor.
A novel selective STAT3 inhibitor that inhibits JAK2-STAT3 activation but has no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src; inhibits STAT3 phosphorylation, dimerization and nuclear translocation, downregulates STAT3-modulated gene expression and induces MM cell apoptosis; delays tumor growth in MM xenograft models (30mg/kg); orally active.