Betaxolol Hydrochloride 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].
Lacidipine-13C8 is the deuterium labeled Lacidipine[1]. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI)[2][3].
Diazoxide-d3 is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A[1]. Lactacystin inhibits cell growth and induces neurite outgrowth[2].
PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively[1].
3-O-Methylquercetin tetraacetate is an antiplatelet agent. 3-O-Methylquercetin tetraacetate has potent antiplatelet effect on arachidonic acid, collagen-induced and PAF-induced platelet aggregation[1].
LAS-31180 is an inhibitor of phosphodiesterase 3, with positive inotropic and vasodilator properties.
JAG-1, scrambled is a scrambled sequence of JAG-1. JAG-1, scrambled with a random sequence of the amino acids that are the same as the active fragment. JAG-1, scrambled usually used as a negative control[1].
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant[1].
SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure[1].
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ[1][2][3][4].
Tetrahydrozoline (hydrochloride) is a α-adrenoceptor agonist. Target: α-adrenoceptorahydrozoline is an imidazoline derivative with alpha receptor agonist activity widely available in over-the-counter topical ocular and nasal formulations. More than 1,600 cases of oral exposures are reported to United States poison centers annually (1,2). Reports of significant toxicity from tetrahydrozoline ingestion are unusual but have occured primarily in small children after unintentional ingestion (3-63, 6) [1].
N-Acetylprocainamide is a class III antiarrhythmic, which blocks K+ channels.
Tirofiban (L700462) hydrochloride is a Gp IIb/IIIa receptor antagonist of nonpeptide derivative of tyrosine. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area[1][2].
SDZ-WAG994 (WAG-994) is a stable, long-acting, selective and orally active A1-adenosine receptor agonist with a KD of 23 nM. SDZ-WAG994 can be used for the research of atrial fibrillation[1].
PCSK9-IN-1 is a novel and highly potent cyclic peptide PCSK9 inhibitor with a Ki value of 1.46 nM.
(-)-Chromanol 293B is a potent and selective inhibitor of the slow component of delayed rectifier K+ current (IKs). (-)-Chromanol 293B can be used for the research of antiarrhythmic[1].
PCSK9-IN-16 is a potent PCSK9 inhibitor. PCSK9-IN-16 is extracted from patent WO2020150474, example 87, has the potential for hypercholesterolemia and other cardiovascular diseases research[1].
19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC50 value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels[1].
Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation[1][2].
Methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone9 is an antagonist of angiotensin II receptor (IC50=48.2 μM). Methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone9 is a quinolone alkaloid from Evodia rutaecarpa[1].
GF109 is a potent parenteral inhibitor of angiotensin converting enzyme (ACE). GF109 has antihypertensive effects[1].
Bradykinin (2-9) is an amino-truncated Bradykinin peptide. Bradykinin (2-9) is a metabolite of Bradykinin, cleaved by Aminopeptidase P.
TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
Norepinephrine bitartrate monohydrate is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.Target: β1- adrenergic receptorNebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Nebivolol treatment for 7 days causes significant reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM, repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48 hours induces a moderate apoptosis of 23% and a decrease from 16% to 5% in the number of cells in S-phase. During Nebivolol incubation, NO formation of HaCEs increases, while endothelin-1 transcription and secretion are suppressed.Administratiion of Nebivolol (initially by iv within 10 minutes of reperfusion and then orally) to rats with myocardial infarction (MI) reduces myocardial apoptosis, which is mediated by regulation of NO . Nebivolol, significantly, prevents left ventricular (LV) pressure changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol treatment lowers mean blood pressure (MBP) in rats with MI slightly, but not significantly.
Fendiline is a nonselective calcium channel blocker.
SQ 26655 is a TxA2 receptor agonist. SQ 26655 induces human platelet aggregation[1].