PeptideDB

AZD-0284

CAS: 2101291-07-8 F: C21H18F6N2O5S W: 524.43

AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis v
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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.