1404380-58-0
Chemical Structure
JTE-151
- CAS No.: 1404380-58-0
- Formula:C28H37ClN2O4
- Molecular Weight:501.06
InChIKey: YWTJAGLMNTUIMB-YSIASYRMSA-N
SMILES: ClC1=CC(C)=CC=C1NC(C[C@H](CCC(O)=O)C2=NOC([C@@H]3C[C@H](CC(C)(C)C)C3)=C2C4CC4)=O
Biological Activity: JTE-151 is an orally active, selective RORγ antagonist with IC50 values of 20.6 nM, 41.8 nM and 32.2 nM against hRORγ, rRORγ and mRORγ, respectively. JTE-151 reduces the production of IL-17. JTE-151 alleviates paw swelling and bone destruction in arthritis models. JTE-151 can be used in research related to rheumatoid arthritis, collagen-induced arthritis, experimental autoimmune encephalomyelitis, psoriasis, multiple sclerosis and inflammatory bowel disease[1][2][3][4].
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JTE-151 | 99.34% | JTE-151 is an orally active, selective RORγ antagonist with IC50 values of 20.6 nM, 41.8 nM and 32.2 nM against hRORγ, rRORγ and mRORγ, respectively. JTE-151 reduces the production of IL-17. JTE-151 alleviates paw swelling and bone destruction in arthritis models. JTE-151 can be used in research related to rheumatoid arthritis, collagen-induced arthritis, experimental autoimmune encephalomyelitis, psoriasis, multiple sclerosis and inflammatory bowel disease. | ||||||||||||||||||||
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- [1]. Arita K, et al. Suppressive Effects of JTE-151, a Novel Orally Available RORγ Antagonist, in Experimental Models of Rheumatoid Arthritis. Biological & pharmaceutical bulletin. 2025;48(7):1118-1124. [Content Brief]
- [2]. Arita K, et al. Pharmacological Properties of JTE-151; A Novel Orally Available RORγ Antagonist That Suppresses Th17 Cell-Related Responses in Vitro and in Vivo. Biol Pharm Bull. 2024;47(12):2050-2057. [Content Brief]
- [3]. Maeba T, et al. Discovery and SAR of JTE-151: A Novel RORγ Inhibitor for Clinical Development. Journal of medicinal chemistry. 2024 Jan 25;67(2):952-970. [Content Brief]
- [4]. Takiguchi H, et al. Practical Synthesis of Chiral 3-(Hydroxyiminomethyl) adipic Acid, a Key Intermediate of the ROR-γ Inhibitor JTE-151, via Crystallization-Induced Dynamic Resolution[J]. Organic Process Research & Development, 2023, 27(12): 2355-2364.
Keywords
