JTE-151 | RORγ inhibitor | Probechem Biochemicals

Chemical Structure : JTE-151

JTE-151 (JTE151)

Catalog No.: PC-20043Not For Human Use, Lab Use Only.

JTE-151 (JTE151) is a potent, selective RORγ antagonist with EC50 of 13 nM in RORγ luciferase assays.

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Biological Activity

JTE-151 (JTE151) is a potent, selective RORγ antagonist with EC50 of 13 nM in RORγ luciferase assays.

JTE-151 demonstrated >100-fold selectivity toward RORγ against 12 nuclear receptors (mGR, hAR, hERα, hPR, hVDR, hFXR, mLXRα, hPPARα, hPPARδ, hPPARγ, hRARα, hRXRα)。

JTE-151 at 3 and 10 mg/kg suppressed IL-17 levels in both lymph node and plasma in mice with the myelin oligodendrocyte glycoprotein (MOG35–55)-induced EAE。

JTE-151 suppressed the Th17 cell differentiation in mouse EAE model.

Physicochemical Properties

M.Wt	499.99
Formula	C26H30ClN3O5
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-6-((2-chloro-4-methylphenyl)amino)-4-(4'-cyclopropyl-5-isobutyl-[3,5'-biisoxazol]-3'-yl)-6-oxohexanoic acid

References

1. Masayuki Kotoku, et al. J Med Chem. 2019 Mar 14;62(5):2837-2842.

2. Nadim S Shaikh, et al. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2208-2217.

JTE-151 (JTE151)

Biological Activity

Physicochemical Properties

References

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