Cardiovascular Disease

Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC₅₀s of 490, 711 nM for bovine cardiac and human cardiac, respectively.

Bococizumab (PF-04950615) is an anti-human PCSK9 inhibitory antibody that reduces LDL cholesterol levels. Bococizumab can be used in the research of hypercholesterolemia.

BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with K_is of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.

Salvianolic acid B is an active ingredient of Salvia miltiorrhiza, which has been widely applied in China for the management of various microcirculation-related disorders, such as cardiovascular disease, cerebrovascular disease, and diabetic vascular complication.

Bradykinin is an effective endothelium-dependent vasodilator that can lower blood pressure. Bradykinin can induce contraction of bronchial and intestinal non-vascular smooth muscle, increase vascular permeability, and participate in the mechanism of pain.

(R)-(-)-Phenylephrine hydrochloride is a selective α₁-adrenoceptor agonist with pK_is of 5.86, 4.87 and 4.70 for α_1D, α_1B and α_1A receptors respectively.

Bay K 8644 ((±)-Bay K 8644) is a racemate consisting of two isomers (R)-(+)-Bay-K-8644 and (S)-(-)-Bay-K-8644. Bay K 8644 is a L-type Ca²⁺ channel agonist with an EC₅₀ of 17.3 nM. Bay K 8644 increases Ca²⁺ influx through sarcolemmal Ca²⁺ channels by increasing the open time of the channel. Bay K 8644 has vasoconstrictive effects.

Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties.

Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC₅₀=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC₅₀ of 7.9 μM.

Flavin adenine dinucleotide (FAD) is a redox cofactor, more specifically a prosthetic group of a protein, involved in several important enzymatic reactions in metabolism.

DETA NONOate (NOC 18) is an exogenous nitric oxide (NO) donor. DETA NONOate shows a slow release normal amounts of NO and long-acting.

Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries.

GW7647 is a potent PPARα agonist, with EC₅₀s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.

S-Nitroso-N-acetyl-DL-penicillamine (SNAP) is a nitric oxide donor and acts as a stable inhibitor of platelet aggregation.

Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with K_is of 140 and 110 nM, respectively.

Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium. Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties. Pterostilbene blocks ROS production, also exhibits inhibitory activity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide.

Daidzein is a soy isoflavone, which acts as a PPAR activator.

Palmitic acid-¹³C₁₆ is the ¹³C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells.

L-Aspartic acid is a NMDA receptor agonist and acidic amino acid. L-Aspartic acid has no independent analgesic activity. L-Aspartic acid can antagonize the analgesic effects of D-Aspartic acid and Morphine. L-Aspartic acid regulates polymorph transformation, crystal growth/aggregation and nucleation processes of calcium carbonate, and can serve as a biomineralization template. L-Aspartic acid promotes burst firing of central neurons. L-Aspartic acid can be used in studies related to cerebral ischemia and epilepsy.

Aluminum Hydroxide is an orally active main form of aluminum used as adjuvant. Aluminum hydroxide-based adjuvant researches include the repository effect, pro-phagocytic effect, and activation of the pro-inflammatory NLRP3 pathway. Aluminum Hydroxide also acts as adjuvant to compensate low inherent immunogenicity of subunit vaccines.