RAR-related orphan receptor gamma (RORγ) Inhibitors Library

RORγ is a member of the large nuclear hormone receptor (NHR) family, many of which are controlled by endogenous ligands, and thus the NHR family has gained considerable attention as an attractive drug target. RORγ controls polarization of native CD4 T cells into pro-inflammatory Th17 cells, and its pharmacological antagonism has therapeutic potential for autoimmune diseases. In addition, recent studies suggest that ROR-γ may be a potential therapeutic target for the treatment of liver fibrosis. RORγ is also capable of converting CD4⁺ immune cells into proinflammatory Th17 cells. Interleukin-17 (IL-17) and T helper 17 (TH17) cells play a crucial role in the tissue inflammation. Therefore, prevention of cytokine’s overproduction could regulate immune response.

BOC Sciences has established a library of RORγ inhibitors that use small-molecule inhibitors to perform a local inhibition of RORγ/RORγt, thereby selectively inhibiting aberrant IL-17 cytokines production.

Figure 1. The dichotomous nature of AZ5104 (an EGFR Inhibitor) towards RORγ and RORγT. (Kara, Ke.; et al. 2019)

Library Design

At BOC Sciences, our teams have employed an in silico screening method based on molecular docking approach to generate this library which contains novel chemical structures with well-predicted affinity to the active site

1. A receptor-based virtual screening process is created based on X-ray data for the complexes
2. The compounds in the HTS compound collection have been pre-filtered using BOC Sciences' internal filters and then docked at the active site
3. Then, we conduct an evaluation of the docking model based on the alignment and scoring of reference compounds
4. Finally, the pharmacophore matching to the hit compound from the BOC Sciences Stock has been demonstrated

RORγ 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. IL23/IL17 axis in psoriasis and targeted therapies. (Hélène, Bugaut.; Sélim A. 2021)

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 RAR-related orphan receptor gamma (RORγ) Inhibitors Library design at competitive prices for global customers. Personalized and customized services of RAR-related orphan receptor gamma (RORγ) 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!