cardiac-specific

(R)-MK-0448 is an isomer of MK-0448.MK-0448 is a novel and selective blocker of the Kv1.5 (KCNA5) channel, a key channel involved in cardiac repolarization that is associated with atrial-specific ultra-rapid K+ current I Kur.

MK-0448 is a novel and selective blocker of the Kv1.5 (KCNA5) channel, a key channel involved in cardiac repolarization that is associated with atrial-specific ultra-rapid K+ current I Kur.

CLT-28643 is a potent and specific α5β1-Integrin inhibitor that prevents fibrosis in glaucoma filtration surgery (GFS), inhibits tumor growth and angiogenesis, suppresses fibrosis and inflammation in a bleomycin-induced lung fibrosis model, and improves insulin sensitivity and cardiac function in H9C2 cells from obese mice.

induces phenotypic differentiation

Heart-homing peptide, abbreviated as CRPPR, is a linear peptide consisting of arginine-rich sequences. Identified as a cardiac-homing peptide due to its specific ability to bind to cardiac endothelium, CRPPR has been proposed to interact with Cysteine-rich intestinal protein-2 (CRIP-2) as its receptor. Additionally, this peptide is utilized for binding to liposomes.

Pyrocatechol sulfate, a phenolic metabolite found in human plasma, is associated with the intake of specific foods such as berries and the state of the gut microbiome. It serves as a potential urinary biomarker for kidney function, dialysis clearance rates, whole grain consumption, and regular coffee intake. Additionally, in conjunction with other phenolic sulfates, pyrocatechol sulfate plays a role in regulating various biological functions, including those related to brain health and the rhythmic beating of cardiac cells.

L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.

GSK329 is an effective and selective inhibitor of TNNI3 Interacting Kinase (TNNI3K). GSK329 exhibits positive cardioprotective outcomes in the model of ischemia reperfusion cardiac injury.

DCN1-UBC12-IN-1 is a potent and specific DCN1-UBC12 inhibitor with an IC50 value of 2.86 nM and anti-cardiac fibrogenic activity.

PKCβII Peptide Inhibitor I, a specific PKCβII inhibitor, exhibits cardioprotective properties in a rat cardiac ischemia reperfusion injury model and mitigates vascular endothelial dysfunction [1].

DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor with an IC50 value of 9.55 nM, targeting DCN1-UBC12 interactions and inhibiting Ang II-induced activation of cardiac fibroblasts.

LSD1-IN-34 (Compound 7d) is an orally effective inhibitor of lysine-specific demethylase (LSD) and monoamine oxidase (MAO), exhibiting IC50 values of 4.51 nM for LSD1 and 18.46 nM for MAO A. This compound inhibits activation of neonatal rat cardiac fibroblasts (NRCF) induced by angiotensin II (Ang II) and shows no significant toxicity at 20 μM. LSD1-IN-34 also inhibits the TGFβ Smad signaling pathway, contributing to the improvement of heart failure in mice. Moreover, it demonstrates favorable pharmacokinetic properties in rats.

GSK1702934A, a selective TRPC3 agonist, modulates cardiac contractility and arrhythmogenesis through TRPC3 activation.

Myosin-IN-1 (compound F10), a specific inhibitor of cardiac myosin, acts by stabilizing the cardiac myosin motor domain in its closed biochemical and structural state. It reduces myocardial force production and calcium sensitivity, functioning as a negative inotropic agent. In isolated Langendorff-perfused rat hearts, Myosin-IN-1 decreases stress in myofilaments and diminishes the development of left ventricular pressure. This compound is applicable in heart failure research [1].

MEISi-2 is a specific MEISi inhibitor that inhibits the meis luciferase reporter gene in vitro and induces MEIS-dependent hematopoietic stem cell maintenance and self-renewal, which can be used in research areas such as cardiac injury, hematopoietic problems, bone marrow transplantation and cancer.

WLSEAGPVVTVRALRGTGSW TFA, a cardiomyocyte-specific peptide, exhibits enhanced performance through its expression in exosomes, which notably improves uptake by cardiomyocytes, reduces apoptosis within these cells, and increases cardiac retention after intramyocardial injection in vivo [1] [2].

Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial cells and accumulated in the cytosol in a biphasic manner[1]. During pelleting hypoxia, Ru360 (10 µM) significantly improves cell viability in wild type cardiomyocytes[3]. Ru360 (15-50 nmol/kg) treatment abolishes the incidence of arrhythmias and haemodynamic dysfunction elicited by reperfusion in a whole rat model. Ru360 administration partially inhibits calcium uptake, preventing mitochondria from depolarization by the opening of the mitochondrial permeability transition pore (mPTP)[1]. [1]. G de J García-Rivas, et al. Ru360, a Specific Mitochondrial Calcium Uptake Inhibitor, Improves Cardiac Post-Ischaemic Functional Recovery in Rats in Vivo. Br J Pharmacol. 2006 Dec;149(7):829-37. [2]. M A Matlib, et al. Oxygen-bridged Dinuclear Ruthenium Amine Complex Specifically Inhibits Ca2+ Uptake Into Mitochondria in Vitro and in Situ in Single Cardiac Myocytes. J Biol Chem. 1998 Apr 24;273(17):10223-31. [3]. Lukas J Motloch, et al. UCP2 Modulates Cardioprotective Effects of Ru360 in Isolated Cardiomyocytes During Ischemia. Pharmaceuticals (Basel). 2015 Aug 4;8(3):474-82.

ent-(+)-verticilide is an effective and specific inhibitor of cardiac ryanodine receptor (RyR2) calcium release channels, demonstrating antiarrhythmic properties. It suppresses RyR2-mediated diastolic Ca2+ leak and shows greater potency and a unique action mechanism compared to Dantrolene and Tetracaine. ent-(+)-verticilide serves as a valuable tool for exploring the therapeutic potential of addressing RyR2 hyperactivity in cardiac and neurological conditions [1].

1,2-Dipentadecanoyl-rac-glycerol (DG(15:0 15:0 0:0)) is a compound referenced in studies examining the effect of insulin on the content of 1,2-diacylglycerol in rat hearts. Insulin is observed to increase the amount of 1,2-diacylglycerol containing specific fatty acid compositions in the heart, which may be linked to cardiac contractility.