Benzofurodil is a cardiotonic, which is used for the chronic treatment of congestive heart failure.
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties[1][2][3].
Apratoxin S4 (Apra S4) is a potent Sec61 inhibitor that prevents cotranslational translocation of secretory proteins into the endoplasmic reticulum (ER). Apratoxin S4 has antiviral effects against some flaviviruses with IC50 values ranging from 0.46 nM to 170 nM, and inhibits retinal vascular cell activation by suppressing multiple angiogenic pathways. Apratoxin S4 can be used for the research of viral infections, angiogenic diseases and cancers[1][2].
Factor XI-IN-1 (Compound 27) is a factor XI activation inhibitor with an EC50 of 25.14 nM[1].
UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP)[1].
Zofenopril Calcium(SQ26991) is an antioxidant that acts as an angiotensin-converting enzyme inhibitor.Target: ACEZofenopril is a pro-drug designed to undergo metabolic hydrolysis yielding the active free sulfhydryl compound zofenoprilat, which is an angiotensin converting enzyme (ACE) inhibitor [1]. Zofenopril promotes the regeneration of peripheral nerve injuries in rat models [2]. Zofenopril increases SR calcium cycling and stimulates active calcium uptake into the SR [3].
L-Homocysteine thiolactone hydrochloride is an intramolecular thioester of homocysteine; prevents translational incorporation of homocysteine into proteins.
Guanfacine Hcl, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors. IC50 Value: 31 nM(Kd)Target: Adrenergic ReceptorGuanfacine is a sympatholytic. It is a selective α2A receptor agonist. These receptors are concentrated heavily in the prefrontal cortex and the locus coeruleus, with the potential to improve attention resulting from interaction with receptors in the former. Guanfacine lowers both systolic and diastolic blood pressure by activating the central nervous system α2A norepinephrine autoreceptors, which results in reduced peripheral sympathetic outflow and thus a reduction in peripheral sympathetic tone. From Wikipedia
GSK269962A hydrochloride (GSK 269962 hydrochloride) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A hydrochloride has anti-inflammatory and vasodilatory activities[1].
CGP 20712 A (CGP 20712 mesylate) is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors[1].
Tyrosylhistidine is a dipeptide consisting of tyrosine and histidine (Tyr-His). Tyrosylhistidine is an orally active antihypertensive peptide. Tyrosylhistidine reduces blood pressure in mice in a model of spontaneous hypertension[1].
RXFP1 receptor agonist-2 (Example 124) is a RXFP1 receptor agonist. RXFP1 receptor agonist-2 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1 nM[1].
Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].
Hexanorcucurbitacin D is a cucurbitacin. Hexanorcucurbitacin D can be isolated from Trichosanthes cucumeroides roots. Hexanorcucurbitacin D can be used for the research of cardiovascular disease (CVD)[1].
Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM)[1][2].
VTP-27999 is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.Ic50 value:Target: Renin
Timolol is a β-blocker available for both topical and systemic administration. Topical Timolol is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension. Timolol can also be used for the research of infantile hemangiomas, hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation.Timolol also has cardioprotective effect[1][2].
SA504 is an anticholinergic agent.
O-Desmethyl apixaban is a metabolite of Apixaban (BMS-562247-01)[1]. 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[2].
CGS35066 is a potent and selective aminophosphonate inhibitor of endothelin-converting enzyme-1 (ECE-1). CGS 35066 inhibits the activity of human ECE-1 and rat kidney neutral endopeptidase 24.11 (NEP) in vitro with IC50 values of 22 nM and 2.3 μM, respectively[1].
Bumetanide(Ro 10-6338; PF 1593) is an inhibitor of Na(+)-K(+)-2Cl(-) co-transporter (NKCC) with an IC50 of 0.6 uM.IC50 Value: 0.6 uM [1]Target: NKCC (Na-K-Cl cotransporter)in vitro: Cultured chick cardiac cells possess a Na+K+Cl-co-transport system that is inhibited by the "loop diuretics" bumetanide (IC50 = 0.6 microM). The K0.5 values for Cl- and Na+ activation of thebumetanide-sensitive 86Rb+ uptake are 59 mM and 40mM respectively. Bumetanide also inhibits a 22Na+ uptake component that is suppressed when external Cl- or K+ are substituted by impermeant ions. The ratio of bumetanide-sensitive 86Rb+ to 22Na+ uptake is close to 1. The cardiac Na+/K+/Cl- cotransport is a major uptake pathway for Na+ and K+ [1]. Bumetanide inhibits ouabain-resistant 86Rb(K+) influx with IC50of 0.1, 5.0, and 0.05 microM for J774.2, CT2 and J7H1 macrophages, respectively [2]. in vivo:Intraperitoneal injection of 50 or 100 mg bumetanide/kg body weight resulted in an acute and transient hyperglycaemia. Pretreatment with 240 mg probenecid/kg body weight reduced the diuretic effect but potentiated the hyperglycaemic effect of bumetanide (50 mg/kg body weight). The glucose tolerance was impaired, and there was an elevated serum glucose and glucose/insulin ratio 2 h after a single injection of bumetanide (100 mg/kg body weight) [3].
BMY 45778 is a non-prostanoid prostacyclin mimetic. BMY 45778 inhibits human (IC50 = 35 nM), rabbit (IC50: 136 nM) and rat (IC50 : 1.3 μM) platelet aggregation. BMY 45778 also activates adenylyl cyclase. BMY 45778 is a partial agonist at the prostacyclin receptor[1].
Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic drug. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy[1][2].
Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
Tiapamil hydrochloride is a calcium channel blocker.
Crizanlizumab is an anti-P-selectin monoclonal antibody. Crizanlizumab binds to P-selectin and blocks its interaction with P-selectin glycoprotein ligand 1 (PSGL-1). Crizanlizumab prevents vaso-occlusive crises (VOCs) and can be used for research of sickle cell disease[1][2][3].
SQ-31765 is a benzazepine calcium channel blocker.
HS-1371 is a potent and ATP-competitive RIP3 inhibitor with an IC50 of 20.8 nM[1].
Nifenalol hydrochloride is a β-adrenergic receptor antagonist. Nifenalol hydrochloride induces the Early Afterdepolarization (EAD) effect. EAD is a phenomenon in cardiac electrophysiology that usually occurs during an action potential in ventricular muscle cells and can lead to arrhythmia. The EAD effect of Nifenalol hydrochloride can be blocked by Tetrodotoxin. Nifenalol hydrochloride is used in the study of conditions such as irregular heartbeat or high blood pressure[1].
Veliflapon (BAY X 1005; DG-031) is an orally active inhibitor of the synthesis of the leukotrienes B4 and C4[1]. Veliflapon is shown to be a selective inhibitor of the formation of 5-lipoxygenase-derived metabolites in vitro, without effects on other routes of arachidonic acid metabolism[2].