Heart Failure

B-007 is an AplnR agonist with G protein-biased signaling (EC₅₀ = 11.6 nM). B-007 activates the G protein pathway while abolishing β-arrestin1 and β-arrestin2 signaling. B-007 serves as a scaffold for development of G protein-biased apelin receptor agonists. B-007 can be used for the research of heart failure.

Cyclocreatine phosphate dilithium is a synthetic intracellular energy buffer. Cyclocreatine phosphate dilithium mediates antiproliferative activity in cells with high creatine kinase levels and inhibits solid tumor growth. Cyclocreatine phosphate dilithium maintains adenosine triphosphate (ATP) levels and protects tissues from hypoxia, cellular damage and inflammation during ischemic events. Cyclocreatine phosphate dilithium accumulates in skeletal muscle, reduces muscle phosphocreatine and total creatine levels, and acts both as a bioenergetic/anti-inflammatory agent and an experimental tool for the assessment of ischemic injury. Cyclocreatine phosphate dilithium can be used in studies related to solid tumors, heart failure and ischemia.

M353-0039 is a selective UT-A2 inhibitor with a human IC₅₀ of 0.35 μM. M353-0039 blocks urea transport mediated by UT-A2. M353-0039 can be used for the study of hyponatremia and edema associated with congestive heart failure, nephrotic syndrome, and cirrhosis.

E822-1968 is an UT-A2 inhibitor with a human IC₅₀ of 0.44 μM. E822-1968 blocks urea transport mediated by UT-A2. E822-1968 can be used for the study of hyponatremia and edema associated with congestive heart failure, nephrotic syndrome, and cirrhosis.

Lixazinone (RS-82856) is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC₅₀ value of 22 nM. Lixazinone exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone increases cyclic adenosine monophosphate (cAMP) levels in human platelets, inhibits thrombin-induced aggregation of human platelets, and blocks the photolabeling of PDE3 active sites by [³²P]cGMP. Lixazinone can be used in the research of polycystic kidney disease and congestive heart failure.

GSK3527497 is an orally active TRPV4 inhibitor. GSK3527497 is applicable for the research of heart failure.

MRS2339 is a ribose-modified nucleotide and a nucleotidase-resistant P2 receptor agonist. MRS2339 activates P2X4R. MRS2339 induces ionic currents via P2X receptors, reduces cardiomyocyte cross-sectional area and heart weight/body weight ratio, lacks vasodilatory activity, and extends the lifespan of mice with cardiomyopathy. MRS2339 can be used in research related to heart failure and cardiomyopathy.

HCN-IN-1 is a TLR4 inhibitor and HCN channel modulator with activity against HCN2 and HCN4.HCN-IN-1 inhibits TLR4-mediated alkaline phosphatase (SEAP) signal activity.HCN-IN-1 reduces HCN2 current across tested voltages, shifts voltage-dependent activation to more hyperpolarized potentials, slows activation kinetics, and does not affect deactivation process.HCN-IN-1 blocks HCN4 current.HCN-IN-1 exhibits analgesic, anti-inflammatory, and anti-anginal effects.HCN-IN-1 can be used for the research of inflammatory pain, neuropathic pain, heart failure, inflammation.

IWP-4 (GMP) is the GMP-grade form of IWP-4 (HY-12879). IWP-4 is a Wnt inhibitor with an IC₅₀ of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC₅₀ of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC₅₀ = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure.

ERβ agonist-2 (Page 72) is a selective ERβ agonist with an EC₅₀ of 800 nM or lower. ERβ agonist-2 selectively inhibits T cell activation and/or proliferation, thereby reducing circulating T cell levels in subjects, without exerting significant effects on circulating neutrophil, monocyte or B cell levels. ERβ agonist-2 is applicable to studies of chronic heart failure after myocardial infarction, as well as graft-versus-host disease, multiple sclerosis and experimental autoimmune encephalomyelitis.

Lixazinone (RS-82856) hydrogensulfate is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC₅₀ value of 22 nM. Lixazinone hydrogensulfate exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone hydrogensulfate increases cyclic adenosine monophosphate (cAMP) levels in human platelets, inhibits thrombin-induced aggregation of human platelets, and blocks the photolabeling of PDE3 active sites by [³²P]cGMP. Lixazinone hydrogensulfate can be used in the research of polycystic kidney disease and congestive heart failure.

SAR296968 is a Na⁺/Ca²⁺ exchanger (NCX) subtype inhibitor with an IC₅₀ value of 74 nM against hNCX1. SAR296968 inhibits both forward and reverse modes of NCX current. SAR296968 enhances cardiac contractility and stroke volume. SAR296968 exerts antiarrhythmic effects. SAR296968 is applicable to research related to heart failure.

CP 71362 is a renin inhibitor, a highly potent substrate-analog transition state mimic with antihypertensive properties. CP 71362 exhibits significant inhibitory activity against plasma renin from rats, dogs, and humans (IC₅₀ values are 3 nM, 0.0033 nM, and 20 nM, respectively). CP 71362 reduces the mean arterial pressure of anesthetized and conscious sodium-depleted animals in a dose-dependent manner, and has pharmacokinetic characteristics of rapid elimination and short duration of action. CP 71362 can be used in research related to hypertension and congestive heart failure.

BMS-986331 is an orally active selective N-Formyl Peptide Receptor 2 (FPR2) agonist with an EC₅₀ of 0.5 nM in humans and 1 nM in rats. BMS-986331 activates Gαi2, GαoA, Gα12, Gα13 signaling pathways, recruits β-arrestin1 and β-arrestin2, and inhibits downstream cAMP. BMS-986331 induces the expression and release of the pro-resolution cytokine IL-10. BMS-986331 improves cardiac structure and function in a rat model of heart failure induced by permanent coronary artery occlusion. BMS-986331 can be used for the research of heart failure.

CCG 224061 is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with a IC₅₀ of 0.066 μM. CCG 224061 inhibits GRK activity in cardiomyocytes. CCG 224061 is applicable to research related to heart disease, heart failure, myocardial hypertrophy and hypertension.

CCG 258001 is a GRK inhibitor with IC₅₀ values of 0.29, 51.8, and 33 µM against GRK2, GRK1, and GRK5, respectively. CCG 258001 inhibits GRK activity in cardiomyocytes and other muscle cells. CCG 258001 is applicable to the research of heart diseases, including heart failure, myocardial hypertrophy, and hypertension.

TMA-IN-1 (Compound 7) is a highly potent, orally active and selective TMA Lyase inhibitor with an estimated K_d value of 3.2 μM. TMA-IN-1 reduces Trimethylamine oxide (TMAO) levels. TMA-IN-1 can be used for the research of heart failure.

R9-13 is a fatty acid-conjugated relaxin and an agonist of LGR7 (RXFP1). R9-13 induces sustained pubic symphysis elongation in estrogen-pretreated mice. R9-13 exhibits long-acting pharmacokinetic profiles in rodents, with in vivo activity lasting up to one week after administration. R9-13 can be used in studies related to acute heart failure.

SERCA2a activator 2 (Compound 25) is a potent SERCA2a (cardiac type) activator, which also has an activating effect on SERCA1a (skeletal muscle type). SERCA2a activator 2, under [Ca²⁺]MAX conditions activates the ATPase activity of SERCA2a and promotes Ca²⁺ uptake, with its EC₅₀ values being 4 μM and 0.80 μM respectively. SERCA2a activator 2 also exhibits consistent activating effects under more physiological [Ca²⁺]MID conditions. SERCA2a activator 2 has low cytotoxicity and can be used for research on diseases such as heart failure.

LCB-2122 is an adenosine-like nucleoside analogue bearing a C2'-stereogenic all-carbon quaternary center. LCB-2122 can prevent Doxorubicin (HY-15142A)-induced cardiomyocytes apoptosis with an IC₅₀ of 0.5 μM and prevent Imatinib (HY-15463)-induced apoptosis. LCB-2122 can activate AMPK signaling and induce the phosphorylation of AMPK and its downstream substrate, acetyl-CoA carboxylase (ACC). LCB-2122 can reduce Doxorubicin-induced mitochondrial damage. LCB-2122 can be used for the research of heart failure.