rat inos

GW274150 is an orally active, selective and potent dual inhibitor of NADPH-dependent human nitric oxide synthase (iNOS) (Kd=40 nM) and rat inducible nitric oxide synthase (iNOS).GW274150 has a low activity against endothelial nitric oxide synthase (eNOS) and neuronal nitric oxide synthase (nNOS) in humans and rats. GW274150 showed protective effects in an inflammatory model of acute lung injury.

2-Iminobiotin hydrobromide (Guanidinobiotin) is a cyclic guanidino analog of biotin that acts as a reversible inhibitor of inducible nitric oxide synthase (iNOS) and neuronal NOS (nNOS; Ki of 21.8 and 37.5 μM for mouse iNOS and rat nNOS, respectively).

GW274150 phosphate is a selective, orally active, and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50: 2.19 μM; Kd: 40 nM) and rat iNOS (ED50: 1.15 μM).

L-NIL is a selective nitric oxide synthase (iNOS) inhibitor that reverses burn-induced activation of glycogen synthase kinase-3β in rat skeletal muscle and may slow the progression of squamous cell carcinoma lung.

L-NMMA acetate (Tilarginine acetate) is an inhibitor of nitric oxide synthase of all NOS isoforms (i.e. NOS1, NOS2, and NOS3). The Ki values are 0.18, 0.4, and 6 µM for nNOS, eNOS, and iNOS, respectively.

iNOs-IN-5 (Compound BN-4) is an inhibitor of iNOS with an IC50 value of 0.1707 μM, effectively reducing NO expression in RAW264.7 cells stimulated by LPS (HT-D1056). It further diminishes the expression of ROS and lactate dehydrogenase induced by hypoxic injury, displaying anti-necrotic and anti-apoptotic properties. In an SD rat model, iNOs-IN-5 exhibits neuroprotective effects against cerebral ischemia and is capable of crossing the blood-brain barrier.

PDE1-IN-9 (Compound 7a) is a selective inhibitor of phosphodiesterase 1 (PDE1), targeting PDE1C with an IC50 value of 11 nM. It effectively reduces the mRNA expression of IL-1β, IL-6, TNF-α, and iNOS, while also inhibiting the production of nitric oxide (NO) and reactive oxygen species (ROS). Additionally, PDE1-IN-9 demonstrates good metabolic stability in rat liver microsomes.

COX-2 15-LOX-IN-6 (Compound 5l) is a dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.201 μM and 11.723 μM, respectively. In serum, it suppresses the expression of PGE, TNF-α, IL-6, and iNOS, and demonstrates anti-inflammatory activity in a carrageenan-induced rat edema model.

L-NIL HCl is a relatively selective iNOS inhibitor (IC50s: 0.4-3.3, 8-38, and 17-92 µM for iNOS, eNOS, and nNOS). L-NIL effectively inhibits iNOS both in vitro and in vivo. L-NIL has been used to demonstrate a critical role for iNOS in the immune response

ATV399 is an inhibitor of iNOS dimerization which protects against Cytokine-Induced rat β-cell dysfunction, thereby inhibiting cleaved caspase-9 activation and subsequent β-cell apoptosis induced by a combination of IL-1β, IFN-γ, and high glucose.

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimental autoimmune encephalomyelitis (EAE). It also decreases serum levels of lactate dehydrogenase as well as hepatic lipid peroxidation, oxidative DNA damage, and PARP levels.

2-Iminobiotin (Guanidinobiotin) is a cyclic guanidino analog of biotin and serves as a reversible inhibitor of inducible nitric oxide synthase (iNOS) and neuronal NOS (nNOS), with Ki values of 21.8 μM for mouse iNOS and 37.5 μM for rat nNOS.

GW274150 (dihydrochloride) is a potent and selective inhibitor of human and rat inducible nitric oxide synthase (iNOS), exhibiting oral activity and NADPH-dependence with an IC50 of 2.19 μM and Kd of 40 nM for human iNOS, and an ED50 of 1.15 μM for rat iNOS. It demonstrates reduced effectiveness against endothelial NOS (eNOS) and neuronal NOS (nNOS) in both species, and has shown protective effects in acute lung injury inflammation models [1] [2] [3].

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 the generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation [1] [2].

Isodunnianol exhibits anti-AChE activity with an IC50 value of 13.0 uM; it also exhibits neurite outgrowth-promoting activity at the concentration ranging from 0.1 to 10 uM in the primary cultured rat cortical neurons. Isodunnianol, dunnianol, and Macrant