Ginsenoside Rg5 is the main component of Red ginseng. Ginsenoside blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
Sabiporide hydrochloride is a NHE-1 inhibitor (Ki: 50 nM). Sabiporide hydrochloride has cardioprotective and neuroprotective effects. Sabiporide hydrochloride inhibits glutamate- or NMDA-induced neuronal cell death[1][2].
CGP-53353 (DAPH-7) is an potent PKC inhibitor with IC50s of 0.41 mM and 3.8 mM for PKCβII and PKCβI, respectively. CGP-53353 can inhibit glucose-induced cell proliferation and DNA synthesis in AoSMC and A10 cells. CGP-53353 can be used for researching atherosclerosis of diabetic patients[1].
Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action[1][2][3].
Stepharine, an natural alkaloid, directly interactes with TLR4 and binds to the TLR4/MD2 complex (TLR4 inhibitor). Stepharine possesses anti-aging, anti-viral and anti-hypertensive effects[1].
Betrixaban D6 is a deuterium labeled Betrixaban. Betrixaban is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor[1].
13-Hydroxylupanine (Hydroxylupanine) is the typical alkaloid profile of sweet lupins.13-Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle[1].
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury[1][2].
NLRP3-IN-2, an intermediate substrate in the synthesis of glyburide, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism[1].
Vitamin E, an essential nutrient for humans and animals reproduction, is a lipid-soluble antioxidant. Vitamin E can protect lipids against oxidative stress, and rescue the glutathione (GSH) depletion-induced hypersensitivity of cells to H2O2. Supplementation with Vitamin E increases its levels in cerebrospinal fluid and plasma, as well as reduces Aβ levels, thus beneficially influences oxidative stress in Alzheimer's disease. Vitamin E also has anti-aging effects[1][2][3][4].
Riociguat-d6 (BAY 632521-d6) is the deuterium labeled Riociguat. Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension[1][2].
TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH)[1].
Sorbinicate, a derivative of nicotinic acid, exerts a favourable influence on blood rheology and platelet function[1].
L-Aspartic acid-1,4-13C2 is the 13C-labeled L-Aspartic acid. L-Aspartic acid is is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly.
Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets.
Enecadin is a neuroprotective agent extracted from patent US 8623823 B2.
α-Linolenic acid-13C18 is the 13C labeled α-Linolenic acid. α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer[1].
Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes[1]. Enniatins B decreases the activation of ERK (p44/p42)[2].
Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
α-D-Glucose-1-phosphate disodium hydrate is used as a starting material for synthesis of glucuronic acid. α-D-Glucose-1-phosphate disodium hydrate can be used as a cytostatic compound essential for cardiopathic therapy, as an antibiotic, as an immunosuppressive drug, and as a circulatory system therapy element[1].
Nile Blue Methacrylamide is a Nile Blue-based nanosized pH densor that can be used for simultaneous far-red and near-infrared live bioimaging[1].
E1231 (E-1231) is a small molecule SIRT1 activator with EC50 of 0.83 uM, interactes with recombinant human SIRT1 protein and deacetylated liver X receptor-alpha (LXRα); increases ATP-binding cassette transporter A1 (ABCA1) expression in RAW 264.7 cells dependent on SIRT1 and LXRα, promotes cholesterol efflux and inhibited lipid accumulation in RAW 264.7 cells via SIRT1 and ABCA1; decreases total cholesterol and triglyceride levels in both serum and the liver in golden hamster hyperlipidemia models.
c-Myc inhibitor 6 (compound A102) is a c-Myc inhibitor. c-Myc inhibitor 6 decreases cancer cell viability and degrades c-Myc protein. c-Myc inhibitor 6 can be used for the research of c-Myc imbalance, such as cancer, cardiovascular diseases, and viral infection[1].
Ibutilide Fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm.Target: Calcium ChannelIbutilide is the first 'pure' class III antiarrhythmic drug to become available. Its predominant action is prolongation of the myocardial action potential duration. Intravenous ibutilide 0.01 to 0.025 mg/kg or 1 to 2 mg successfully converted atrial flutter or fibrillation to sinus rhythm in 33 to 49% of patients in 2 placebo-controlled trials involving 439 patients with sustained arrhythmia [1]. Ibutilide appears to be an effective alternative method for rapid conversion of recent-onset AF or AFl. The drug may be particularly useful in patients who have undergone recent cardiac surgery or those who are not ideal candidates for DCC [2].
Canrenoate (Aldadiene) potassium, a prodrug that releases canrenone, is a potent, competitive mineralocorticoid receptor (aldosterone receptor) antagonist. Potassium canrenoate, as a diuretic, is used for the research of hypertension[1][2][3].
Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
VTP-27999 Hcl is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.IC50 value:Target: Renin
Kisspeptin 234, is a 10 amino acid peptide as well as a kisspeptin receptor (KISS1, GPR54) antagonist. Kisspeptin 234 is an analog of Kisspeptin 10[1].
Acipimox is a niacin derivative used as a hypolipidemic agent.Target: Acipimox is a niacin derivative used as a hypolipidemic agent. It is used in low doses and may have less marked adverse effects, although it is unclear whether the recommended dose is as effective as are standard doses of nicotinic acid. Acipimox inhibits the production of triglycerides by the liver and the secretion of VLDL, which leads indirectly to a modest reduction in LDL and increase in HDL. Long-term administration is associated with reduced mortality, but unwanted effects limit its clinical use. Adverse effects include flushing (associated with Prostaglandin D2), palpitations, and GI disturbances. Flushing can be reduced by taking aspirin 20-30 min before taking Acipimox. High doses can cause disorders of liver function, impair glucose tolerance and precipitate gout. From Wikipedia.
Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC50 values of 48.8 μM and 477.5 μM, respectively[1].