Broussonin A is a potent BChE inhibitor, with an IC50 of 4.16 µM. Broussonin A is a diarylpropane natural product that can be isolated from the bark of Broussonetia papyrifera after solid fermentation[1][2][3].
GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4[1].
MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
Stobadine is a potent antioxidant and prevents free radical induced alterations in ER membrane fluidity. Stobadine can be used for effective cardio- and neuroprotectants development based on antioxidant or free radical scavenging mechanisms of action[1].
YM 254890 is a selective Gq signaling inhibitor that strongly inhibits intracellular calcium ion mobilization and serum response element (SRE)-mediated transcription stimulated by several receptors coupled to Gq, but not those coupled to Gi, Gs, or G15; also exhibits antithrombotic and thrombolytic effects in an electrically induced carotid artery thrombosis model in rats; inhibits ADP-induced platelet aggregation in human platelet-rich plasma with an IC50 of <0.6 uM by blocking the P2Y1 receptor-signal transduction pathway. Thrombosis Discontinued
Carpaine is an alkaloid isolated from Carica papaya Linn with anti-thrombocytopenic activity, exhibits potent activity in sustaining platelet counts with no acute toxicity[1].Carpaine has anti-plasmodial activity to prevent malaria[2].Carpaine affects the myocardium directly, it reduces cardiac output, stroke volume, stroke work, and cardiac power in rat, which has been studied for its cardiovascular effects[3].
Pholedrine hydrochloride, the main metabolite of methamphetamine, is an indirectly acting sympathomimetic amine. Pholedrine hydrochloride is a cardiovascular agent exerting hypertensive and adrenergic effects. Pholedrine hydrochloride can produce mydriatic response and allow localization of the site of the interruption in the oculosympathetic pathway. Pholedrine hydrochloride can be used as a topical eye drop and a diagnostic agent for use in Horner's syndrome[1][2][3].
SCH-42354 is a potent, orally active neutral endopeptidase (NEP) inhibitor, is the pharmacologically active form of the prodrug SCH-42495. SCH-42354 inhibits the hydrolysis of NEP to enhance the activity of atrial natriuretic peptide (ANP). SCH-42354 inhibits hydrolysis of leu-enkephalin and ANF with IC50 values of 8.3 nM and 10.0 nM, respectively. SCH-42354 has antihypertensive activity[1][2].
Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
SDF-1α (human) is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) can be used in cardiovascular disease research[1][2].
ROMK-IN-32 is a potent, selective ROMK inhibitor with IC50 of 17 nM; shows an improved functional hERG/ROMK potency ratio (1176x) and preclinical PK profile; demonstrates blood pressure lowering effects in the spontaneously hypertensive rat model.
Magnesium Lithospermate B is a derivative of caffeic acid tetramer and extracted from Salviae miltiorrhizae. Magnesium Lithospermate B is widely used for the research of cardiovascular diseases, and it can protect against glucose-induced intracellular oxidative damage. Magnesium Lithospermate B also suppresses neuroinflammation and attenuates neurodegeneration[1][2][3].
SC40230 is a class I antiarrhythmic agent.
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
Disulfamide, an orally active diuretic, is a carbonic anhydrase inhibitor with the IC50 value of 0.07 μM. Disulfamide leads to diuresis by inhibiting carbonic anhydrase and preventing the reabsorption of sodium and bicarbonate in the proximal tubule[1].
(±)-Coclaurine is a natural product that can be found in Roemeria refracta. (±)-Coclaurine exhibits antioxidative activity and cardiovascular effects[1][2][3].
Indanazoline (as monohydrochloride active substance of Farial) is characterized by a pronounced vasoconstrictive action.
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats[1][2].
AR-C66096 tetrasodium is a selective platelet P2YT receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism[1].
DCN1-UBC12-IN-1 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.86 nM. Anticardiac fibrotic effect[1].
NBTGR (p-Nitrobenzylthioguanosine) is a potent inhibitor of nucleoside transport; inhibits adenosine uptake with a Ki of 70 nM.
Cyclocreatine is a Creatine analogue and acts as a potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine crosses membranes, enters the brain, and can be phosphorylated and dephosphorylated by creatine kinases[1].
Prasugrel hydrochloride is a platelet inhibitor with IC50 value of 1.8 μM.Target: P2Y12 receptorPrasugrel hydrochloride is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI [2].Prasugrel hydrochloride reduces the aggregation ("clumping") of platelets by irreversibly binding to P2Y12 receptors. In rat platelets, prasugrel hydrochloride AM inhibited in vitro platelet aggregation induced by ADP (10 μm) with an IC50 value of 1.8 Μm [2]. Clinical indications: Acute coronary syndrome; Ischemic heart disease; Sickle cell anemia; Stroke; Vascular occlusive diseaseFDA Approved Date: February 2009Toxicity: Hypertension; Headache; Hypercholesterolemia/hyperlipidemia; Nausea; Epistaxis
GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue[1].
Sotalol D6 hydrochloride is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is a non-selective competitive β-adrenergic receptor antagonist that also exhibits Class III antiarrhythmic properties by its inhibition of potassium channels[1][2].
Isoprenaline hydrochloride is a non-selective beta-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities.
Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity[1][2].
AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD)[1].
GKT137831 is a selective NADPH oxidase (NOX1/4) inhibitor with Kis of 140 and 110 nM, respectively.
Deferitrin (GT-56-252), a desferrithiocin (DFT) analogue, is an orally active trident iron chelator. Deferitrin is used for chronic iron overload due to transfusional therapy. Deferitrin has the potential for beta-thalassemia major[1][2].