NO Synthase Inhibitor

Myoglobin is an oxygen-binding heme protein. Myoglobin scavenges ROS via its peroxidase activity, and binds to and inactivates NO in the heart and oxidative skeletal muscle. Myoglobin stores, buffers and facilitates intracellular oxygen diffusion, maintains aerobic metabolism under hypoxic/anoxic conditions, and provides oxygen supply support for mitochondria. Myoglobin alleviates oxidative stress, protects cardiac function and affects cardiac redox pathways. Myoglobin can be used in studies related to ischemia-reperfusion injury, oxidative stress-induced cardiac dysfunction and acute myocardial infarction.

Protegrin-1 is an orally active antibacterial peptide. Protegrin-1 activates ERK, COX2, NFκB, inhibits Apoptosis, and NO production. Protegrin-1 has antibacterial activity against S. aureus, E. faecium, E. coli, P. aeruginosa and K. Pneumoniae, with MBC values between 10 and 20 µM. Protegrin-1 has antiviral activity against dengue NS2B-NS3. Protegrin-1 has anti-inflammatory activity. Protegrin-1 is used in the study of inflammatory diseases and infections.

Isobavachin is an orally active, blood-brain barrier-penetrating prenylated flavonoid present in Psoralea corylifolia. Isobavachin inhibits human CYP2B6, CYP2C9, CYP2C19, UGT1A1, UGT1A9, and UGT2B7. Isobavachin suppresses MAPK activation, NF-κB nuclear translocation, overexpression of iNOS/COX-2, FcεRI-mediated signaling pathways, and RANKL-induced osteoclastogenesis. Isobavachin induces autophagy, cytotoxicity, neuronal differentiation, and NRF2 activation; it alleviates oxidative damage, inflammatory responses, apoptosis, iron accumulation, mitochondrial biogenesis, and mast cell degranulation. Isobavachin is applicable to research related to liver injury, inflammatory diseases, osteoporosis, liver cancer, prostate cancer, glioma, periodontitis-induced bone loss, and Alzheimer's disease.

Myricitrin, a naturally occurring flavonoid, is an orally active nitric oxide (NO) and PKC inhibitor. Myricitrin has central nervous system activity, including anxiolytic-like action. Myricitrin possesses antioxidant, anti-inflammatory, antifibrotic and anti-malarial effects.

Gluconate sodium (D-Gluconic acid sodium salt) is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury.

2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with K_is of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively. 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage.

Royal Jelly Acid ((E)-Queen Bee Acid) is a major fatty acid found in royal jelly with oral bioavailability, exhibiting anti-inflammatory, anticancer, antimalarial, antiprotozoal, and neuroregulatory activities. Royal Jelly Acid can be used for research in various fields, including cancer, infections, immune inflammation, and neurological diseases.

Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC₅₀ of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.

7-Nitroindazole is a selective and BBB-penetrable inhibitor of nitric oxide synthase (NOS) (IC₅₀ = 0.47 μM in mouse cerebellum). 7-Nitroindazole does not affect blood pressure or endothelium-dependent relaxation while inhibiting nNOS in experimental animals. 7-Nitroindazole has anti-injurious and neuroprotective properties, and can be studied in research for neurological diseases such as Parkinson’s disease.

Harpagoside can be obtained by Harpagophytum procumbens, which has anti-inflammatory, anti-cancer, protective activity, and efficacy. Harpagoside has an inhibitory effect on COX-1 and COX-2 active, and suppresses NO production. Harpagoside inhibits HepG2 cell lipid polysaccharide, which is a protein that is expressed horizontally and selectively, and has anti-inflammatory and latent pain effects. Harpagoside has the ability to protect the body, and has a degenerative effect on the β-oxidation (Aβ).

Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.

GW274150 is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC₅₀=2.19 μM; K_d=40 nM) and rat iNOS (ED₅₀=1.15 μM). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation.

L-Canavanine sulfate is a selective inhibitor of inducible NO synthase.

Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling.

Diisononyl phthalate (DINP) is an orally active polyvinyl chloride plasticizer and indirect food additive. Diisononyl phthalate activates the ACE/AT1R axis and inhibits the production of NO. Diisononyl phthalate reduces the expression of eNOS. Diisononyl phthalate induces increased blood pressure in mice. Diisononyl phthalate induces monocytic leukemia in rats. Diisononyl phthalate can be used in hypertension-related research.

Oxiracetam (ISF2522) is an orally active and a BBB-penetrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases .

Monoolein is a biocompatible lipid molecule that can be used as a carrier for bone repair. Monoolein exhibits anti-inflammatory activity by inhibiting the immune response induced by LPS (HY-D1056). It exerts its anti-inflammatory effects by reducing the production of immune response factors such as IL-12 p40, IL-6, and TNF-α, and inhibiting the generation of NO. Monoolein can be used in drug delivery and research in the field of inflammatory diseases .

Gluconate (D-Gluconic acid) Calcium is an orally active glucose derivative. Gluconate Calcium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate Calcium inhibits ERK phosphorylation. Gluconate Calcium has antioxidant and antiplatelet activation activities. Gluconate Calcium has antitumor activity against colorectal cancer. Gluconate Calcium improves osteoarthritis, intestinal damage and acute lung injury.

1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a K_d value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation.

Callistephin (Pelargonidin 3-O-glucoside) chloride is an anthocyanin. Callistephin chloride regulates the expression of inflammatory (reducing iNOS/TNF-α/COX-2) and apoptosis-related proteins by inhibiting p38 phosphorylation, and enhances the protective effect of Isoflurane (HY-A0134) on microglial cell damage. Callistephin chloride significantly reduces ROS levels, eliminates DPPH free radicals, protects retinal pigment epithelial cells, and inhibits lipid peroxidation. Callistephin chloride can alleviate glutamate excitotoxicity, reduce neuronal apoptosis, and protect cerebellar granule neurons. Callistephin chloride can inhibit the proliferation and metastasis of breast cancer cells by inducing apoptosis.