Cardiovascular Disease

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

Methylprednisolone (U 7532) is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.

Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC₅₀ of 195 nM. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

ODN 1826 is a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist. ODN 1826 induces NO and iNOS production and enhances Apoptosis. ODN 1826 enhances immune surveillance. ODN 1826 increases aortic atherosclerotic plaque size. ODN 1826 has antitumor activity against lung cancer, glioma and melanoma.

Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC₅₀ of 20 nM.

Finerenone (BAY 94-8862) is a third-generation, selective, and orally active nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀ = 18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (> 500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.

GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca²⁺ influx and elevate intracellular Ca²⁺ in HEK cells.

Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.

Norepinephrine (Levarterenol; L-Noradrenaline) hydrochloride is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α₁, α₂, β₁ receptors.

GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC₅₀s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.

Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.

Puerarin is an isoflavone extracted from Pueraria root and is a 5-HT2C receptor antagonist. Puerarin inhibits the dorsal motor nucleus of the vagus (DMV)-vagus nerve pathway, which in turn leads to decreased fat absorption.

L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca⁺ channels antagonist with a K_i of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (K_B of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.

(R)-GNE-140 is a potent inhibitor of lactate dehydrogenase (LDH) A, B and C, with IC₅₀ values of 3, 5 and 5 nM against LDHA, LDHB, LDHC, respectively. (R)-GNE-140 blocks the conversion of pyruvate to lactate, reduces lactate production and histone lysine lactylation, and inhibits glycolysis. (R)-GNE-140 attenuates cardiac hypertrophy, alleviates PM_2.5-induced pulmonary inflammation and fibrosis, blocks MRSA-induced Arg1 expression. (R)-GNE-140 is applicable to research related to pathological cardiac hypertrophy, pulmonary fibrosis, MRSA infection and pancreatic cancer.

Heparin is a highly sulfated glycosaminoglycan,that is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule. Heparin significantly inhibits exosome-cell interactions.

GCN2iB is an ATP-competitive, selective GCN2 inhibitor with an IC₅₀ of 2.4 nM. GCN2iB inhibits the activation of the GCN2 pathway and upregulates GPX4. GCN2iB enhances the anticancer effect of ASNase against acute lymphoblastic leukemia. GCN2iB increases left ventricular ejection fraction, while reducing fasting blood glucose and myocardial fibrosis. GCN2iB can be used in research related to acute lymphoblastic leukemia, acute myeloid leukemia and diabetic cardiomyopathy.

Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC₅₀ values of 0.39 and 0.71 nM for Human mAChR M₄ and Chicken mAChR M₄, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia.

α-CGRP (human) (Calcitonin gene-related peptide) is a regulatory neuropeptide of 37 amino acids. α-CGRP (human) is widely distributed in the central and peripheral nervous system. α-CGRP (human) is a potent vasodilator and has inotropic and chronotropic effects.

Angiotensin II human (Angiotensin II) acetate is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human acetate plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis. Angiotensin II human acetate induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.