Cardiovascular Disease

Evans Blue (Direct Blue 53; T-1824; C.I. 23860) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability.

Monensin (Monensin A) sodium, an orally active antibiotic, is an ionophore that mediates Na⁺/H⁺ exchange. Monensin sodium is a potent Wnt signaling inhibitor. Monensin sodium causes a marked enlargement of the multivesicular bodies (MVBs) and regulates exosome secretion. Monensin sodium can be used for bacterial, fungal, and parasitic infections research, and shows anticancer effects.

Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC₅₀=1 pM) than ROCK1 (IC₅₀=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC₅₀ of 150 nM.

L-Ascorbic acid sodium salt (Sodium ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt selectively inhibits Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.

4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.

D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β₃-adrenergic receptor (β₃-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.

Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC₅₀ of 74 pM.

Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.

(R)-(-)-Phenylephrine is a selective α₁-adrenoceptor agonist primarily used as a decongestant.

Chlorogenic acid is a major phenolic compound in Lonicera japonica Thunb. It is an orally active antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension compound.

Intralipid 20% is a safe fat emulsion, composed of soybean oil (consisting of a mixture of long-chain triglycerides (C14-24) of predominantly unsaturated fatty acids), and egg phospholipids, can be used as a nutritional supplement. Intralipid 20% effectively inhibits the opening of the mitochondrial permeability transition pore, effectively protecting the heart from ischaemia-reperfusion injury and has some potential to modulate the innate immune response.

Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with K_is of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.

Zenidolol (ICI-118551) hydrochloride is a highly selective β2 adrenergic receptor antagonist, with K_is of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

Poloxamer 407 (F127) is a nonionic surfactant that is 100% active and relatively non-toxic to cells at low concentrations, and frequently used with dye AM esters such as Indo-1 AM, Fura-2 AM, Calcein AM, Fluo-3 AM, Fluo-4 AM, Quest Fluo-8 AM and Quest Rhod-4 AM, etc. to improve their water solubility. Poloxamer 407 is also a lipoprotein lipase inhibitor.

Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study.

Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor. Zinc Protoporphyrin regulates expression of HO-1 at the transcriptional level. The effect of Zinc Protoporphyrin on HO-1 expression is controversial.  It was shown to induce HO-1 expression in some cells, but suppress it in others. Zinc Protoporphyrin is used as a screening marker of iron deficiency in vivo. Zinc Protoporphyrin has anti-cancer activity.

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.

MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin and promotes its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells.

Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.