NO Synthase Inhibitor

Ethyl Caffeate is a natural phenolic compound isolated from Bidens pilosa. Ethyl caffeate suppresses NF-κB activation and its downstream inflammatory mediators, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and prostaglandin E2 (PGE2) in vitro or in mouse skin.

SARS-CoV-2-IN-107 (Compound A7) is the inhibitor for SARS-CoV-2 3CLpro with an IC₅₀ of 261.3 nM. SARS-CoV-2-IN-107 inhibits the SARS-CoV-2 replication with an EC₅₀ of 11.7 μM. SARS-CoV-2-IN-107 exhibits anti-inflammatory activity with a NO inhibition rate of 68.6% in LPS (HY-D1056)-stimulated RAW264.7 macrophages.

Apterin is a natural compound with anti-inflammatory activity. Apterin shows significantly inhibitory activity on NO production in RAW264.7 cells with an IC₅₀ value of 41.8 μM.

Leupeptin hydrochloride is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hydrochloride significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hydrochloride inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hydrochloride can be used in research on chronic inflammatory diseases and skin tumorigenesis.

13 (S)-HOTrE is an oxylipin metabolite of α-Linolenic acid (HY-N0728). 13 (S)-HOTrE mediates the inactivation of the NLRP3 inflammasome through the PPAR-γ pathway to exert anti-inflammatory effects. 13 (S)-HOTrE inhibits NF-κB nuclear translocation, ROS production, autophagy and IL-1β levels, induces apoptosis, and increases IL-10 levels. 13 (S)-HOTrE alleviates LPS-induced inflammatory responses in macrophages, prolongs the survival time of septic mice, and regulates the immunometabolic phenotype in parenteral nutrition mouse models. 13 (S)-HOTrE can be used in the research of immune and inflammation-related diseases.

2,4-Diamino-6-hydroxypyrimidine (Standard) is the analytical standard of 2,4-Diamino-6-hydroxypyrimidine. This product is intended for research and analytical applications. 2,4-Diamino-6-hydroxypyrimidine is a specific GTP cyclohydrolase I inhibitor (the rate-limiting enzyme in de novo pterin synthesis). 2,4-Diamino-6-hydroxypyrimidine blocks Tetrahydrobiopterin (BH4) synthesis and suppresses NO production.

BYK 191023 is a selective and L-arginine competitive inducible nitric-oxide synthase inhibitor with an IC₅₀ value of 86 nM, 17 µM, 162 µM for inducible (iNOS), neuronal (nNOS), and endothelial (eNOS) NO synthases respectively.

Saquinavir (Standard) (Ro 31-8959 (Standard)) is the analytical standard of Saquinavir (HY-17007). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

TLR4-IN-2 (Compound Racemic-11k) is inhibitors of TLR4, JNK, and NF-κB. TLR4-IN-2 inhibits NO production in LPS-stimulated RAW264.7 cells with an IC₅₀ value of 23.2 µM. TLR4-IN-2 exerts anti-inflammatory activity by inhibiting TLR4 expression, reducing JNK phosphorylation, thereby suppressing the activation of NF-κB, blocking the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and decreasing the production of inflammatory mediators such as NO, PGE 2, and TNF-α. TLR4-IN-2 is promising for research of inflammatory diseases, such as rheumatoid arthritis and various inflammatory disorders.

Carboxy-PTIO (potassium) (Standard) is the analytical standard of Carboxy-PTIO (potassium). This product is intended for research and analytical applications. Carboxy-PTIO potassium is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO potassium can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model.

Isoacteoside (Standard) is the analytical standard of Isoacteoside. This product is intended for research and analytical applications. Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products. Isoacteoside Standard regulates the AKT/PI3K/m-TOR/NF-κB signaling pathway, induces apoptosis in OVCAR-3 cell. Isoacteoside Standard exhibits antitumor, anti-inflammatory, anti-obesity and neuroprotective activities.

9-Hydroxy-α-lapachone (α-Dihydrocaryopterone) is a natural phenol, exhibits potent inhibitory effects with an IC₅₀ of 4.64 µM on LPS-induced NO production in RAW 264.7 cells.

Dehydroevodiamine Standard is the analytical standard of Dehydroevodiamine (HY-N2106). This product is intended for research and analytical applications. Dehydroevodiamine is a blood-brain barrier-permeable, orally effective AChE and BACE1 inhibitor (IC₅₀ = 40.96 μM). Dehydroevodiamine is isolated and extracted from Evodia rutaecarpa. Dehydroevodiamine attenuates neurotoxicity through multiple targets by inhibiting BACE1 to block Aβ production, inhibiting AChE activity, scavenging ROS, and suppressing calcium influx. Dehydroevodiamine can be used for research on Alzheimer's disease, cerebral ischemia, vascular dementia, and other cognitive disorder-related diseases.

Oxiracetam (Standard) is the analytical standard of Oxiracetam. This product is intended for research and analytical applications. 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.

Swertianolin (Standard) is the analytical standard of Swertianolin (HY-N2192). This product is intended for research and analytical applications. Swertianolin is a xanthone glycoside. Swertianolin can be isolated from plants of the Gentianaceae family (e.g., Gentiana campestris and Swertia punicea). Swertianolin inhibits p38 phosphorylation and NF-κB activation, and reduces NO and ROS production. Swertianolin exhibits anti-Helicobacter pylori activity with an IC₅₀ of 6.1 μM and a minimum bactericidal concentration of 91.7 μM. Swertianolin modulates immune function in sepsis. Swertianolin is useful in the research of diseases such as Alzheimer's disease, hepatitis B, Helicobacter pylori infection, and sepsis.

Notoptetherin D is a coumarin compound isolated from the roots and rhizomes of Notopterygium incisum. Notoptetherin D inhibits nitric oxide (NO) production in LPS (HY-D1056A1)-induced RAW 264.7 cells, with an IC₅₀ of 20.4 μM. Notoptetherin D suppresses nitric oxide generation.

Necrosulfonamide (Standard) is the analytical standard of Necrosulfonamide (HY-100573). This product is intended for research and analytical applications. Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.

1,3-PBIT is a potent inhibitor of iNOS with a Ki of 47 nM compared to Ki values for eNOS and nNOS are 9 and 0.25 μM, respectively, for the purified human enzymes. Its inhibition in whole cells is greatly diminished, presumably to poor membrane permeability.

Indigoticoside A is a phenylpropanoid lignan natural product that can be found in the traditional Chinese medicine Banlangen (Isatis indigotica Fort.), with antioxidant and anti-inflammatory activities. Indigoticoside A scavenges DPPH free radicals, superoxide anions and hydroxyl radicals in a dose-dependent manner, exhibiting significant in vitro antioxidant effects. The blood-absorbed components of Banlangen containing Indigoticoside A inhibit LPS (HY-D1056)-induced inflammatory responses in macrophages and reduce the production of inflammatory mediators such as NO, PGE₂ and TNF-α.

Paroxetine (BRL29060) acetate is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine acetate inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine acetate is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine acetate is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.