myocardial

GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

Mexiletine hydrochloride (KOE-1173 hydrochloride) is a voltage-gated sodium channel blocker and a Class IB antiarrhythmic drug. Mexiletine hydrochloride exerts antiarrhythmic effects by inhibiting sodium current in myocardial cells, thereby reducing the rise rate of cardiac action potential (phase 0) and reducing the automaticity of Purkinje fibers.

Amrinone (Inocor) is a positive inotropic cardiotonic (cardiotonic agent) with vasodilator properties, phosphodiesterase 3 inhibitory activity.

Isosorbide dinitrate (Isordil) is a vasodilator used in the treatment of angina pectoris.

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide), an intermediate capable of synthesizing glibenclamide, exerts an inhibitory effect on the formation of NLRP3 inflammatory vesicles in cardiomyocytes, limiting infarct size after myocardial ischemia/reperfusion in mice and has no effect on metabolism.

Trimethylamine N-oxide dihydrate (TMANO dihydrate) is a gut microbiota-dependent metabolite derived from dietary choline and other trimethylamine-containing nutrients. It induces inflammation by activating the ROS/NLRP3 inflammasome and promotes fibroblast differentiation and cardiac fibrosis via the TGF-β/Smad2 signaling pathway. TMANO dihydrate can be used to establish models of cardiac hypertrophy and cardiac fibrosis.

VULM 1457 is a potent ACAT inhibitor. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells.

Resorcinolnaphthalein is a specific enhancer of angiotensin-converting enzyme 2 (ACE2) (EC50 value of 19.5 μM).

DG-041 is an antagonist of high-affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively). DG-041 inhibits PGE2 facilitation of platelet aggregation and has the blood-brain barrier permeability.

AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.

SB 204741 is a selective 5-HT2B antagonist with high affinity and pKi value of 7.1.

Losartan Carboxylic Acid (E-3174), a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), produces a depressor response and vasodilatation. As a metabolite of losartan, it is more potent than losartan in blocking angiotensin II-induced responses in vascular smooth muscle cells.

Binodenoson (WRC 0470) is a potent and selective A2A adenosine receptor agonist (KD=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging[1].

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain to interfere with its homodimerization and suppress MyD88 signaling. TJ-M2010-5 can be used in myocardial [ischemia/reperfusion] injury studies.

Gap19 is a peptide that corresponds to a sequence on the cytoplasmic loop (CL) of Cx43.

Timolol is a nonselective beta-adrenergic receptor blocker that is widely used for the therapy of hypertension, angina pectoris and prevention of vascular headaches.

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

Indacaterol (Onbrez; Arcapta) is a β2-Adrenergic Agonist. The mechanism of action of indacaterol is as an Adrenergic beta2-Agonist.

Temocapril is an inhibitor of tyrosine kinase.

Bisoprolol, a selective beta-1 adrenergic receptor antagonist, selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, thereby with antihypertensive activity and devoid of intrinsic sympathomimetic activity.

Indacaterol maleate (QAB149) is an ultra-long-acting β-adrenoceptor agonist.

Bisoprolol is a cardioselective β1-adrenergic blocker used for secondary prevention of heart failure, myocardial, angina pectorisinfarction (MI) and mild to moderate hypertension.

Regadenoson (CVT-3146) is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors.