NO Synthase Inhibitor

GABAAR/5-HT2AR modulator-1 is an orally active and brain-penetrant GABA_AR agonist and 5-HT_2AR antagonist with K_d values of 0.89 and 0.78 μM. GABAAR/5-HT2AR modulator-1 blocks 5-HT-stimulated IP1 accumulation, inducing a chloride current, reduces LPS (HY-D1056)-induced increases of ROS, NO, TNF-α, IL-6, IL-1β, iNOS, and COX-2 levels. Antidepressant agent 11 dihydrochloride inhibits NF-κB pathway activation by reducing IκBα and p65 phosphorylation and blocking p65 nuclear translocation. GABAAR/5-HT2AR modulator-1 alleviates depression-like behaviors in LPS-challenged and chronic restraint stress-challenged mice, and protects hippocampal neurons against inflammation-mediated damage.

11-Deoxyalisol B, a triterpene, shows the potent inhibitory activity on Lipopolysaccharide (LPS)-induced nitric oxide (NO) production.

Isolupalbigenin is an inhibitor of NO. Isolupalbigenin has anti-proliferative activity on HL-60 cells with an IC₅₀ of 5.1 μM.

Paroxetine-d6-1 (BRL29060-d6-1) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine 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 is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine 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.

O-Acetylschisantherin L (Acetylschisantherin L) is a natural lignan, which exhibits inhibitory effects on LPS-induced NO production in BV-2 cells with an IC₅₀ of 23.1 μM.

PI3K/AKT-IN-6 is an orally effective PI3K/AKT signaling pathway inhibitor and anti-inflammatory agent. PI3K/AKT-IN-6 inhibits the production of pro-inflammatory cytokines TNF-α and IL-6, and downregulates the expression of inflammatory mediators COX-2 and iNOS. PI3K/AKT-IN-6 improves related symptoms in colitis mice. PI3K/AKT-IN-6 can be used for the research of inflammatory diseases such as colitis.

Papiliocin is a potent peptide antibiotic with both anti-inflammatory and antibacterial activities. Papiliocin is primarily active against Gram-negative bacteria. Papiliocin exhibits strong anti-inflammatory activity against cell, exerting its anti-inflammatory activity by inhibiting the production of NO and the secretion of TNF-α and MIP-2. Papiliocin participates in the innate defense response mechanism by inhibiting the Toll-like receptor pathway and NF-κB. Papiliocin induces apoptosis in fungal cells and increases the total level of intracellular ROS. Papiliocin acts as an effective antiseptic peptide in sepsis models. Papiliocin is useful in anti-inflammatory and antibacterial research.

NOS-IN-3 (Compound 9a) is a potent, selective, imidamide derived NOS inhibitor with an IC₅₀ against iNOS of 4.6 μM, without inhibiting eNOS. NOS-IN-3 has little toxicity and can be studied in the research of inducible isoform involved diseases, such as septic shock.

HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC₅₀ of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy.

(±)-Eudesmin ((±)-Eudesmine) is a natural compound found in Fragaria nubicola with in vitro anti-inflammatory activity. (±)-Eudesmin inhibits NO production in LPS-activated macrophages; suppresses myeloperoxidase-dependent ROS production in zymosan-activated phagocytes; and inhibits superoxide anion production in PMA-activated macrophages. (±)-Eudesmin can be used for the research of inflammation-related diseases.

Anti-inflammatory agent 19 (compound 2b) shows NO inhibitory activity, with an IC₅₀ of 36.00 μM. Anti-inflammatory agent 19 inhibits HMGB1-induced later inflammation. Anti-inflammatory agent 19 can be used for the research of later inflammation diseases such as coronavirus diseases (COVID-19) and sepsis, etc.

Sodium propionate-¹³C-2 is the ¹³C-labeled Propionate sodium (HY-B1773A). Sodium propionate is an orally active short-chain fatty acid. Sodium propionate can be produced by intestinal bacteria from the metabolism of dietary fiber. Sodium propionate increases PPAR-γ, inhibits NF-κB activation, and reduces COX-2 expression and NO production. Sodium propionate also induces Apoptosis and Autophagy. Sodium propionate reduces HSV-1-induced keratitis. Sodium propionate has anticancer effects against glioblastoma. Sodium propionate exhibits neuroprotective, antioxidant, and anti-inflammatory activities. Sodium propionate can be used in the research of spinal cord injury and Alzheimer's disease.

Valeriandoid F is an iridoid, which potently inhibits NO production with an IC₅₀ value of 0.88 μM. Valeriandoid F has anti-inflammatory and antiproliferative activities.

Britannilactone diacetate (1,6-O,O-Diacetylbritannilactone; Compound 2) exhibits potential NO inhibition effect. Britannilactone diacetate exhibits activity against NO production induced by LPS in BV-2 microglial cells with the EC₅₀ value of 6.3 μM. Britannilactone diacetate exhibits a favorable blood-brain barriers (BBB) penetration and absorption, distribution, metabolism, excretion, and toxicity (ADMET) property.

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

Desmethoxyyangonin (Standard) is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin (Standard) is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC₅₀: 0.123  µM). Desmethoxyyangonin (Standard) exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin (Standard) induces CYP3A23 expression and leads to skeletal muscle relaxation.

Kazinol B, a prenylated flavan with a dimethyl pyrane ring, is an inhibitor of nitric oxide (NO) production. Kazinol B improves insulin sensitivity by enhancing glucose uptake via the insulin-Akt signaling pathway and AMPK activation. Kazinol B has the potential for diabetes mellitus research.

Avanafil-¹³C₅ (TA1790-¹³C₅) is ¹³C labeled Avanafil. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC₅₀ values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.

α-Gracinoic acid is a Chalcone (HY-121054) derivative with anti-inflammatory activity. α-Gracinoic acid inhibits nitric oxide production catalyzed by inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-treated RAW 264.7 cells.

Mycosporine 2 glycine is an anti-inflammatory agent and TYRP1 inhibitor. Mycosporine 2 glycine inhibits the expression of inflammatory genes and reduces nitric oxide production. Mycosporine 2 glycine binds tightly to the active pocket of TYRP1 and inhibits the activity of melanogenesis-related enzymes. Mycosporine 2 glycine can be used in the research of hyperpigmentation and inflammation-related diseases.