S18-000003 is a potent, effective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of 29 nM. S18-000003 inhibits Th17 cells from naive CD4+T cells. S18-000003 inhibits IL-17 production in the skin of IL-23-treated mice in a dose-dependent manner.
|Solubility (25°C)||DMSO 100 mg/mL|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Chihiro Imura, et al. J Dermatol Sci. A novel RORγt inhibitor is a potential therapeutic agent for the topical treatment of psoriasis with low risk of thymic aberrations
 Yoshikazu Sasaki, et al. Bioorg Med Chem Lett. Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor, S18-000003
|Related ROR Products|
Dehydrolithocholic acid is a bile acid metabolite, which inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
Zilovertamab (UC-961) is a humanised monoclonal antibody against ROR1 that blocks Wnt5a-induced ROR1 signalling.
SHR168442 is a modulator of RORγ with an IC50 value of 0.035 μM. It can be used as a skin-restricted topical compound for the study of psoriasis.
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist.
Neoruscogenin is a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (NR1F1).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.