Regaloside C is a glycerol glucoside isolated from the bulbs of Lilium genus with anti-inflammatory activities. Regaloside C has cardiomyocyte protective activity by protecting the mitochondria in H2O2-induced heart H9C2 cells[1].
Darusentan is a selective endothelin A (ETA) receptor antagonist. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM[1].
C-Type Natriuretic Peptide (1-53), human is the 1-53 fragment of C-Type Natriuretic Peptide. C-Type Natriuretic Peptide is natriuretic peptide family peptide that is involved in the maintenance of electrolyte-fluid balance and vascular tone[1].
Big Endothelin-1 (22-38), human is derived from human, is the 22-38 fragment of Big Endothelin-1 (ET-1) (1-38). Big ET-1 (1-38) is a propeptide of ET-1, which has potent and long-lasting vasoconstrictor effects, equips a specific enzymatic cleavage of the 38 amino acid chain to form ET-1 (1-21) and the C-terminal fragment Big ET-1 (22-38)[1].
2R,4R-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect[1][2][3].
RXFP1 receptor agonist-4 (Example 268) is a RXFP1 receptor agonist. RXFP1 receptor agonist-4 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 4.9 nM[1].
Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate is a prodrug of pindolol and can be used for essential and renovascular hypertension research[1][2].
CAY 10465 is a selective and high-affinity AhR agonist, with a Ki of 0.2 nM, and shows no effect on estrogen receptor (Ki >100000 nM).
Yohimbic acid is an amphoteric demethylated derivative of Yohimbine. Yohimbic acid exhibits vasodilatory action, and has the potential for osteoarthritis (OA) research[1][2][3].
Hydrangetin inhibits platelet aggregation. Hydrangetin can be isolated from Zanthoxylum schinifolium[1].
MGV354 is a novel potent, selective soluble Guanylate Cyclase (sGC) activator, lowers intraocular pressure (IOP) in preclinical models of glaucoma. Other Indication Phase 2 Clinical
PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
Orbofiban is an orally active platelet GPIIb/IIIa antagonist that inhibits platelet aggregation.
GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
Nexopamil racemate is the racemate of Nexopamil. Nexopamil is a combined Ca2+/5-HT2 antagonist on thrombus formation in vivo and on platelet aggregation in vitro.
YM-244769 hydrochloride is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice[1][2][3].
Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline nitrate can be used for non-bacterial conjunctivitis research[1][2].
Dronedarone hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
Mephentermine (hydrochloride) can increase peripheral resistance significantly. Mephentermine (hydrochloride) can be used in the research of cardiovascular areas[1].
Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel vasoselective Ca2+ channel antagonist.
PI3K-IN-46 (Intermediate 4) is an intermediate in the synthesis of PI3K inhibitor (2-imino-azolinone-vinyl fused-benzene derivative) that can be used for the research of autoimmune disorders, cardiovascular diseases, and neurodegenerative diseases[1].
Mavacamten-d1 (MYK461-d1; SAR439152-d1) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor for the research of acute ischemic stroke[1].
Trimazosin is an orally active, quinazoline derivative which is structurally related to prazosin. Trimazosin shows hypotensive effect by selectively block α1-adrenoceptors[1][2].
Protokylol (Caytine; JB-251) is a beta-adrenergic receptor agonist and TRPV1 agonist. Protokylol is used as a bronchodilator[1].
2-MPMDQ is a potent and selective α1-adrenoceptor (Ki=0.37 nM) antagonist over α2-adrenoceptor (Ki=1740 nM). 2-MPMDQ is potent anti-hypertensive agent and has the potential for hypertension research[1].
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessel in vivo. RWJ-56110 induces cell apoptosis[1][2].
Dopexamine hydrochloride is a β2 adrenergic receptor agonist.
Linoleic acid-13C18 is the 13C labeled Linoleic acid. Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism [1][2].