AL 082D06

• CAT Number: I002875
• CAS Number: 256925-03-8
• Molecular Formula: C23H24ClN3O2
• Molecular Weight: 409.91
• Purity: ≥95%
• Target: GR antagonist
• Solubility: DMSO: ≤ 7.5 mg/mL
• Storage: Store at +4C
• IC50: 210 nM(Ki) [2]
• InChI: InChI=1S/C23H24ClN3O2/c1-25(2)18-9-5-16(6-10-18)23(17-7-11-19(12-8-17)26(3)4)21-15-20(27(28)29)13-14-22(21)24/h5-15,23H,1-4H3
• InChIKey: IPICUXHYPAMJNC-UHFFFAOYSA-N
• SMILES: CN(C)C1=CC=C(C(C2=CC=C(N(C)C)C=C2)C3=CC([N+]([O-])=O)=CC=C3Cl)C=C1

AL 082D06 (D-06)(CAT: I002875) stands as a pioneering compound in the realm of pharmaceutical and endocrine research. As the first selective, nonsteroidal glucocorticoid receptor (GR) antagonist, it holds a significant position in the development of targeted therapies. With a remarkable Ki value of 210 nM, AL 082D06 effectively competes for binding to the GR, offering potential applications in modulating the glucocorticoid signaling pathway. Notably, its excellent selectivity against androgen receptor (AR), progesterone receptor (PR), mineralocorticoid receptor (MR), and estrogen receptor (ER) (Ki > 10 µM) highlights its specificity for the GR.

Reference

[1]. Avenant C, et al. Role of ligand-dependent GR phosphorylation and half-life in determination of ligand-specific transcriptional activity. Mol Cell Endocrinol. 2010 Oct 7;327(1-2):72-88.
[2]. Miner JN, et al. A nonsteroidal glucocorticoid receptor antagonist. Mol Endocrinol. 2003 Jan;17(1):117-27.