Vimirogant is a RORγ inhibitor, which has a Ki value of <100 nM. Vimirogant is used for the research of treating autoimmune disorders, including multiple sclerosis and psoriasis.
|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.
|Solubility||DMSO 10 mM|
Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc) Inhibitors: Hits and Misses.
Pandya VB, et al. J Med Chem. 2018 Dec 27;61(24):10976-10995. PMID: 30010338.
RORγt inhibitors as potential back-ups for the phase II candidate VTP-43742 from Vitae Pharmaceuticals: patent evaluation of WO2016061160 and US20160122345.
Gege C, et al. Expert Opin Ther Pat. 2017 Jan;27(1):1-8. PMID: 27852111.
Retinoid-related orphan receptor gamma t (RORγt) inhibitors from Vitae Pharmaceuticals (WO2015116904) and structure proposal for their Phase I candidate VTP-43742.
Gege C. Expert Opin Ther Pat. 2016 Jun;26(6):737-44. PMID: 26895086.
|Related ROR Products|
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.
Neoruscogenin is a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (NR1F1).
GSK805 is a potent, orally bioavailable RORγγ Inhibitor, with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
SR2211 is a synthetic RORγ-selective modulator, functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
SR 1001 is a RORα/γ inverse agonist with Ki values of 172 and 111 nM, respectively.
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