Neophytadiene is a diterpene found in Turbinaria ornate, with anti-inflammatory antioxidant and cardioprotective properties[1].
L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively[1]. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6[2]. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases[1][2][3].
Limaprost-d3 (17α,20-dimethyl-δ2-PGE1-d3) is the deuterium labeled Limaprost. Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research[1][2].
Thrombin inhibitor 1 is a potent thrombin inhibitor (Ki=0.66 nM, 2xaPTT=0.43 μM).
Glenzocimab (ACT017) is a Fab fragment of humanized anti-GPVI monoclonal antibody. Glenzocimab inhibits collagen-induced platelet aggregation. Glenzocimab has the potential for the research of acute ischemic stroke[1][2].
Glycerol derivative 1 is a Glycerol derivative extracted from patent EP 672415 A1, compound (1).
Desglymidodrine (ST 1059), the active metabolite of midodrine, is a selective α1-adrenoceptor agonist. Desglymidodrine is an effective arterial and venous vasoconstrictor and can be used to regulate blood pressure[1][2].
LY-517717 is a potent and orally active FXa inhibitor. LY-517717 shows antithrombotic and anticoagulant activity. LY-517717 has the potential for the research of venous thromboembolism after hip or knee replacement[1].
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors[1].
TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM[1]. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons[2].
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
Methyldopate is an ethyl ester prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate has the potential for severe hypertension research [1].
Auriculin A is a synthetic atrial natriuretic factor (ANF) with hemodynamic effect. Auriculin A antagonizes renal vasoconstriction in the dog, and influences on arterial baroreflex control of heart rate, systemic blood pressure, and perfusion pressure in the hind limb (perfused at constant flow) in rabbits[1][2].
Lercanidipine-d3 hydrochloride is the deuterium labeled Lercanidipine. Lercanidipine is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine has long lasting antihypertensive action and reno-protective effect[1][2][3].
Tanshinone IIB is a major active constituent of the roots of Salvia miltiorrhiza (Danshen) widely used for the research of stroke and coronary heart disease in Asian countries. Tanshinone IIB has a neuroprotective effect via inhibition of apoptosis[1].
Lomitapide-d8 is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Abanoquil (U-K52046), an potent and selective α-1 adrenoceptor antagonist, is an anti-arrhythmic agent. Abanoquil can be used for erectile dysfunction research[1][2].
Semastatin 5A.1 is an anti-angiogenic 19-amino acid peptides that are derived from proteins containing type I thrombospondin motifs[1].
Trimetazidine-d8 dihydrochloride is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.
Adrenotensin (human) (Pro-ADM-153-185 (human)) is a 153-185 fragment of precursor peptide of Adrenomedullin. Adrenomedullin (ADM) is a 52-amino acid multifunctional peptide, which belongs to the CGRP superfamily of vasoactive peptide hormones[1].
CAY 10434 dihydrochloride is a potent CYP4A hydroxylase inhibitor. CAY 10434 dihydrochloride improves contractile response to angiotensin II with the maximal contractile response (Emax) 6764 mg[1].
Ro 22-9194 inhibits aggregation and thromboxane Az (TXA2) synthetase activity in rabbit and human platelets. Ro 22-9194 has a potent inhibitory action against various types of model arrhythmias. Ro 22-9194 has non-cholinergic cardiac depressant properties with its vasodilating action[1][2].
Methionylserine (H-MET-SER-OH) is a methionine- and serine-containing dipeptide. Methionylserine binds to and translocation via intestinal di/tri-peptide transporter 1 (hPEPT1) with a Km value of 0.2 mM. Methionylserine inhibits ACE enzyme activity. Methionylserine can be used in the research of hypension[1][2].
Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1).
Pronethalol-d6 ((±)-Pronethalo-d6) is the deuterium labeled Pronethalol. Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs)[1][2][3].
(3S,5R)-Fluvastatin sodium ((3S,5R)-XU 62-320) is the (3S,5R)-enantiomer of Fluvastatin. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
CCG-271423 is a potent and selective GRK5 inhibitor with IC50 values of 0.0021 μM and 44 μM for GRK5 and GRK2, respectively. CCG-271423 inhibits cardiomyocyte contractility and decreases in Ca2+ transience[1].
Temocapril Hydrochloride is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension. Target: ACETemocapril hydrochloride is a novel prodrug-type angiotensin-I converting enzyme (ACE) inhibitor, lowering of the dose of temocapril might be recommended only in patients with severe renal insufficiency [1]. Temocapril is regarded as an ACE inhibitor the disposition and efficacy of which are little affected in patients with impaired liver function [2].
Vitexin is a c-glycosylated flavone, and is found in various medicinal plants species such as Ficus deltoid and Spirodela polyrhiza. Vitexin has a wide range of pharmacological effects, including anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects[1][2].