XY018

XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM) . XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) [1].

Product Specifications

CAS Number

[1873358-87-2]

UNSPSC

12352005

Target

ROR

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/xy018.html

Purity

99.68

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC(C(F)(F)F)(C1=CC(F)=C(C(C=C2)=CC=C2NC(CC(C=CC=C3)=C3[N](=O)=O)=O)C=C1)C(F)(F)F

Molecular Formula

C23H15F7N2O4

Molecular Weight

516.37

References & Citations

[1]Junjian Wang, et al. ROR-γ Drives Androgen Receptor Expression and Represents a Therapeutic Target in Castration-Resistant Prostate Cancer. Nat Med. 2016 May;22 (5) :488-96.|[2]Yan Zhang, et al. Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer. J Med Chem. 2019 May 9;62 (9) :4716-4730.