NO Synthase Inhibitor

NLRP3-IN-76 is an orally active NLRP3 inhibitor. NLRP3-IN-76 inhibits the production of NO, and the mRNA levels of proinflammatory cytokines (iNOS, IL-6, IL-1β and TNFα). NLRP3-IN-76 shows anti-inflammatory effects by inhibiting the activation of the NLRP3 inflammasome and NF-κB signaling pathway. NLRP3-IN-76 ameliorates DSS (HY-116282C)-induced colitis and can be used for research of inflammatory bowel diseases (IBD).

Dimeric coniferyl acetate is a NO production inhibitor with an IC₅₀ value 7.9 μM in BV-2 microglial cells.

Isosilychristin is a P-glycoprotein inhibitor with an IC₅₀ of 25.9 μM. Isosilychristin downregulates the expression of transmembrane efflux pumps, exerts intracellular antioxidant effects, and inhibits NO production in macrophages. Isosilychristin regulates cell cycle progression, and exerts weak antiproliferative and colony formation inhibitory effects in prostate cancer cells. Isosilychristin reduces bacterial intercellular communication and reverses the drug resistance of Staphylococcus aureus. Isosilychristin can be used in studies related to prostate cancer, inflammation and bacterial infections.

Akt/NF-κB/MAPK-IN-1 (compound 2m) is a potent and orally active inhibitor against NO (IC₅₀=7.70 μM) with no significant toxicity. Akt/NF-κB/MAPK-IN-1 shows anti-inflammatory activity by inhibiting Akt/NF-κB and MAPK signaling pathways.

rel-Cleroindicin F (Rengyolone) is a cyclohexyl acetyl compound that can be isolated from the fruit of forsythia and has anti-inflammatory activity. It strongly inhibits the production of nitric oxide (NO) and tumor necrosis factor-alpha (TNF-α). rel-Cleroindicin F does this by downregulating the activity of NF-κB and NF-κB kinases in RAW 264.7 cells stimulated by LPS (HY-D1056), thus inhibiting the expression of inducible nitric oxide synthase (NO Synthase) and nitric oxide production.

Pulegone-d₈ is deuterated labeled Pulegone (HY-N1500). Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.

Avanafil-d₄ (TA1790-d₄) is deuterium-labeled Avanafil (HY-18252).

Rhodomollein XI is a naturally occurring grayanane diterpenoid with anti-inflammatory and analgesic activities. Rhodomollein XI inhibits LPS-induced NO production in RAW264.7 mouse macrophages. Rhodomollein XI exhibits analgesic effects in the mouse acetic acid-induced writhing test. Rhodomollein XI can be used for pain- and inflammation-related research.

N1-Acetyl-5-methoxykynuramine hydrochloride (AMK hydrochloride) is an active metabolite of Melatonin (HY-B0075) with antioxidant activity and blood-brain barrier permeability. N1-Acetyl-5-methoxykynuramine hydrochloride inhibits LPS-induced activation of inducible nitric oxide synthase and COX-2, scavenges ROS, hydroxyl radicals, carbonate radicals and ABTS cation radicals, and protects bovine serum albumin from peroxyl radical-mediated damage. N1-Acetyl-5-methoxykynuramine hydrochloride reduces the increase in cytoplasmic and mitochondrial lipid peroxidation in the substantia nigra and striatum in MPTP (HY-15608)-induced mouse models of Parkinson's disease. N1-Acetyl-5-methoxykynuramine hydrochloride can be used in studies related to Parkinson's disease, metabolism-related diseases and oxidative stress.

2,4-Dihydroxy-6-methoxy-3,5-diprenylacetophenone (Compound 8) is an Acetophenone (HY-Y0989) derivative found in Acronychia oligophlebia. 2,4-Dihydroxy-6-methoxy-3,5-diprenylacetophenone exhibits anti-inflammatory and antioxidant activities. 2,4-Dihydroxy-6-methoxy-3,5-diprenylacetophenone can inhibit LPS (HY-D1056)-induced NO production (IC₅₀ = 34.5 μM) and scavenge DPPH free radical (SC₅₀ = 0.15 mM). 2,4-Dihydroxy-6-methoxy-3,5-diprenylacetophenone can be used for the research of inflammation.

(±)-Methotrexate-¹³C,d₃ disodium ((±)-Amethopterin-¹³C,d₃ disodium; (±)-CL14377-¹³C,d₃ disodium; (±)-WR19039-¹³C,d₃ disodium) is the deuterated, ¹³C-labeled (±)-Methotrexate (HY-121151). (±)-Methotrexate is the racemate of Methotrexate (HY-14519). Methotrexate is an orally active antifolate (Antifolate). Methotrexate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.

1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one is an inhibitor of iNOS and COX-2. 1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one inhibits LPS-induced excessive production of NO and PGE₂, as well as the mRNA expression of pro-inflammatory cytokines TNF-α, IL-1β, IL-6 and IL-12. 1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one can be used in inflammation-related research.

Circumdatin C is an alkaloid. Circumdatin C shows inhibitory effects against LPS-stimulated NO production. Circumdatin C inhibits AChE activity with an IC₅₀ value of 13.9 μM. Circumdatin C can be used in the research of Alzheimer's disease.

(+)-Hannokinol can be isolated from AMOMUM TSAO-KO (ginger family) fruit. (+)-Hannokinol inhibits lipopolysaccharide-induced nitric oxide production in BV2 microglia.

12-Acetoxyganoderic acid D is a triterpenoid compound found in Ganoderma sinense. 12-Acetoxyganoderic acid D exhibits certain anti-inflammatory activity and inhibits NO production in LPS (HY-D1056) stimulated RAW 264.7 macrophages.

Butyrolactone Ia is the inhibitor for the NO production with an IC₅₀ of 18 μM. Butyrolactone Ia inhibits LPS (HY-D1056)-induced mRNA expression of iNOS and the inflammatory cytokine IL-1β. Butyrolactone Ia modulates autophagy in HeLa cells, and exhibits immune suppressive activity.

Guanidino ethyl disulfide (GED) (Compound 23) is a NO Synthase (NOS) inhibitor with EC₅₀s of 110, 630 and 180  μM for iNOS, eNOS and bNOS, respectivly. Guanidino ethyl disulfide effectively inhibits nitrite production in J774.2 macrophages. Guanidino ethyl disulfide can be used for circulatory shock, inflammation and neurological diseases research.

5-LOX/NO-IN-1 (Compound 7e) is a 5-LOX and NO release inhibitor. 5-LOX/NO-IN-1 shows an IC₅₀ of 2.833 μM for 5-LOX. 5-LOX/NO-IN-1 has anti-inflammatory effects.

Anti-inflammatory agent 23 (Compound 4m) is an anti-inflammatory agent. Anti-inflammatory agent 23 inhibits the production of NO activated by LPS with an IC₅₀ of 0.449 μM. Anti-inflammatory agent 23 has a good affinity for p65 protein.

Kansuinine E is a plant-derived nitric oxide inhibitor (IC₅₀=6.3 μM). Kansuinine E belongs to jatrophane-type diterpenoids and is isolated from the roots of E. kansui.