Nitric Oxide Synthase Inducible (iNOS) Inhibitors Library

The vast majority of human diseases have an inflammatory component, and a key mediator of immune activation and inflammation is inducible nitric oxide synthase, which produces nitric oxide (NO) from L-arginine. Dysregulation or overexpression of iNOS can increase the level of NO, and this increased NO level is associated with complex multifactorial diseases such as Parkinson's disease, Alzheimer's disease, multiple sclerosis, rheumatoid arthritis, and inflammatory bowel disease. Selective inhibition of iNOS is an effective approach in treatment of such complex diseases. L-Arginine, a substrate for iNOS, is a natural lead for the development of iNOS inhibitors. A number of potent iNOS inhibitors have been identified that show promising potential in animal models of endotoxemia, inflammatory and neuropathic pain, arthritis and other diseases.

Withe the goal of helping the medicinal chemists for rational designing of novel and potent iNOS inhibitors, BOC Sciences has developed a iNOS Inhibitors library.

Figure 1. Regulation of iNOS activity by the availability of its substrate L-Arginine. (Cinelli, M.; et al. 2020)

Library Design

• We screen the BOC Sciences HTS compound collection by using three known isoforms in mammals (two are constitutive (cNOS) and the third one is inducible (iNOS))
• The well-developed model contains obligatory interactions with two key-role residues in the active site and/or metal-binding ability
• iNOS binding site surface with docking constraints covers both the re-docked inhibitor from crystal structure, and one of the compounds from the BOC Sciences HTS compound collection

iNOS Inhibitors Library Characteristics

• Favorable physicochemical parameters and solubility requirements
• No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
• Bioactivity and safety confirmed by preclinical studies and clinical trials
• Structural diversity, medicinal activity, and cellular penetration
• Structural document, IC₅₀, and other chemical and biological data are provided
• All compounds are continually updated
• Compound cherry-picking service is provided

Figure 2. Different mechanisms by which COX-2 derived prostaglandins are involved in the carcinogenesis. (Cinelli, M.; et al. 2020)

What We Deliver

• Delivered within 2 weeks in any customer-preferred format
• Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
• All compounds have a minimum purity of 90% assessed by ¹H NMR and HPLC
• Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of Nitric Oxide Synthase Inducible (iNOS) Inhibitors Library design at competitive prices for global customers. Personalized and customized services of Nitric Oxide Synthase Inducible (iNOS) Inhibitors Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!