Cardiovascular Disease

Fucoidan, a biologically active polysaccharide, is an efficient inhibitor of α-amylase and α-glucosidase. Anticoagulant, antitumor, antioxidant and antisteatotic activities.

Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.

Dehydroascorbic acid is an oxidized form of vitamin C that can cross the blood-brain barrier (BBB). Dehydroascorbic acid clears cytotoxic reactive oxygen species (ROS) produced after ischemic stroke by converting to ascorbic acid (AA), thereby reducing neuronal and glial cell damage and stabilizing cerebral microvascular NO signaling to maintain perfusion in the ischemic area. Dehydroascorbic acid can be used in research on ischemic stroke.

PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC₅₀ of 2 nM and a K_i of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC₅₀ of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.

Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with K_d of 0.6-1.1 μM in the presence of CO.

Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC₅₀ of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities.

Syrosingopine (Su 3118) is an orally active lactate transporters (MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality in cancer cells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine.

Lycopene is naturally occurring carotenoids found in tomato, tomato products, and in other red fruits and vegetables; exhibits antioxidant effects.

Dipyridamole is an orally active phosphodiesterase (PDE) inhibitor. Dipyridamole also is an antiplatelet agent used in secondary prophylaxis against stroke. Dipyridamole can induce cancer cell-specific apoptosis.

Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.

Dexamethasone (Hexadecadrol) Water Soluble is a water-soluble form of Dexamethasone (HY-14648). Dexamethasone is a glucocorticoid receptor agonist, apoptosis inducer, and a common disease inducer in experimental animals. It can be used to construct models of muscle atrophy, hypertension, and depression. Dexamethasone can inhibit the production of inflammatory miRNA-155 exosomes in macrophages and significantly reduce the expression of inflammatory factors in neutrophils and monocytes. Dexamethasone also has the potential to be used in COVID-19 research.(Sale size is the weight of dexamethasone)

Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.

GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.

Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab is used in the study of hypercholesterolemia and atherosclerotic cardiovascular disease. Evolocumab binds to circulating PCSK9 protein and inhibits its binding to LDLR. Evolocumab has antioxidant and cytoprotective activities against H₂O₂-induced oxidative damage to endothelial cells. Evolocumab may also negatively regulate activation of the TLR-4/NF-κB signaling pathway to prevent inflammation.

Tetrazolium Red (2,3,5-Triphenyltetrazolium chloride; TTC) is a not brain-penetrant, colorless, water-soluble dye that is reduced by mitochondrial enzymes to a deep red, water-insoluble compound (formazan) mainly in the mitochondria of living cells. Tetrazolium Red is used to observe the activity of dehydrogenase, and it turns colorless to red when exposed to hydrogen. Tetrazolium Red distinguishes between surviving and infarcted brain tissue after stroke. Tetrazolium Red has been used to stain heart tissue to measure the extent of acute lesions and also used to stain brain tissue to detect the size of the infarcted area. The absorption wavelength of Tetrazolium Red is 570 nm.

Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.

MG149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC₅₀ of 74 uM, similar potentcy for MOF (IC₅₀ = 47 uM); little potent for PCAF and p300 (IC₅₀ >200 uM). MG 149 inhibits KAT8 and blocks PINK1 kinase activity. MG149 inhibits the phosphorylation of Parkin and ubiquitin, thereby suppressing the initiation of PINK1-dependent mitophagy. MG 149 can reverse chronic restraint stress (CRS) induced hypertension and related molecular changes. MG 149 commonly used in research on diseases such as hypertension and Parkinson's disease.

Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC₅₀ of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.

6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.

7-Ketocholesterol is an oxidation product of cholesterol, widely present in atherosclerotic plaques, and has a stronger atherogenic effect than cholesterol. 7-Ketocholesterol can inhibit the rate-limiting enzymes involved in bile acid and cholesterol synthesis, such as cholesterol 7α-hydroxylase and HMG-CoA reductase. 7-Ketocholesterol exhibits pro-inflammatory effects both in vivo and in vitro and can induce cell apoptosis (apoptosis).