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Vimirogant

Cat. No. M9265
Vimirogant Structure
Synonym:

AGN-242428; VTP-43742; RORγ-IN-1

Size Price Availability
1mg USD 800  USD800 Custom Synthesis
5mg USD 2700  USD2700 Custom Synthesis
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 552.65
Formula C27H35F3N4O3S
CAS Number 1802706-04-2
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] Pandya VB, et al. J Med Chem. Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc) Inhibitors: Hits and Misses.

[2] Gege C, et al. Expert Opin Ther Pat. RORγt inhibitors as potential back-ups for the phase II candidate VTP-43742 from Vitae Pharmaceuticals: patent evaluation of WO2016061160 and US20160122345.

[3] Gege C. Expert Opin Ther Pat. Retinoid-related orphan receptor gamma t (RORγt) inhibitors from Vitae Pharmaceuticals (WO2015116904) and structure proposal for their Phase I candidate VTP-43742.

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  Catalog
Abmole Inhibitor Catalog




Keywords: Vimirogant, AGN-242428; VTP-43742; RORγ-IN-1 supplier, ROR, inhibitors, activators


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