2998548-65-3
2998548-65-3
Chemical Structure
SJPYT-331
- CAS No.: 2998548-65-3
- Formula:C26H32N4O6
- Molecular Weight:496.56
SMILES: COC1=C(N2C(C)=C(N=N2)C(NC3=C(C=CC(C(OC)=O)=C3)O[C@@H](CC)CCC)=O)C=C(C=C1)OC
Biological Activity: SJPYT-331 is a potent and selective PXR antagonist with an IC50 of 7.1 nM. SJPYT-331 exerts its antagonistic effect on PXR by targeting and binding to the PXR ligand-binding pocket (IC50 = 3.6 nM) and inducing conformational destabilization of the core helix α12 in the AF-2 region, thereby hindering coactivator recruitment. SJPYT-331 can be used for research on PXR-related metabolic diseases[1][2].
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SJPYT-331 | SJPYT-331 is a potent and selective PXR antagonist with an IC50 of 7.1 nM. SJPYT-331 exerts its antagonistic effect on PXR by targeting and binding to the PXR ligand-binding pocket (IC50 = 3.6 nM) and inducing conformational destabilization of the core helix α12 in the AF-2 region, thereby hindering coactivator recruitment. SJPYT-331 can be used for research on PXR-related metabolic diseases. | |||||||||||||||||||||
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References
- [1]. Garcia-Maldonado E, et al. Chemical manipulation of an activation/inhibition switch in the nuclear receptor PXR. Nature communications. 2024 May 14;15(1):4054. [Content Brief]
- [2]. Kamaraj R, et al. Discovery of PXR antagonist MI891 and PXR degrader MI1013 and their roles in hepatic gene regulation. Journal of Medicinal Chemistry. 2025 Jul 24;68(14):14271-99. [Content Brief]
