Bioactivity | AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment[1]. |
Target | pIC50: 7.4 (FRET RORγ) |
Invitro | AZD0284 (0.37 μM; 5 days) inhibits IL-17A production in human TH17 cells[1].AZD0284 reduces polarization of TH17 into pathogenic TH17/1 cells. AZD0284 decreases frequency of single IL-17+cell as well as double positive TH17/1 cells. AZD0284 reduces IL-17A secretion and RNA expression of IL-17A, IL-17F, IL-22 and IL-23R[1][2]. |
Name | AZD-0284 |
CAS | 2101291-07-8 |
Formula | C21H18F6N2O5S |
Molar Mass | 524.43 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
Reference | [1]. Narjes, F, et al. The discovery of AZD0284, an inverse agonist of the nuclear receptor RORg. American Chemical Society, 2017 Drug Design and Delivery Symposium 26 October 2017 [2]. Asimus S, et al. Pharmacokinetics, pharmacodynamics and safety of the inverse retinoic acid-related orphan receptor γ agonist AZD0284 [published online ahead of print, 2020 Feb 17]. Br J Clin Pharmacol. 2020;10.1111/bcp.14253. |