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2,2,2-trifluoro-N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]acetamide

Names

[ CAS No. ]:
1034148-04-3

[ Name ]:
2,2,2-trifluoro-N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]acetamide

[Synonym ]:
Acetamide, 2,2,2-trifluoro-N-[(1S,2R)-2-[[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy]-2-(3-methoxyphenyl)-1-methylethyl]-
unii-641h0q518w
2,2,2-Trifluoro-N-[(1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-(3-methoxyphenyl)-2-propanyl]acetamide
AZD5423
AZD-5423

Biological Activity

[Description]:

AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM)[1]. AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma[2].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor

[Target]

Glucocorticoid receptor[1]


[In Vitro]

The affinity of AZD5423 to the glucocorticoid receptor is high with an IC50 of 0.9 nM in a radioligand human glucocorticoid receptor assay, and selectivity towards other steroid hormone receptors is >900-fold[1].

[References]

[1]. Werkström V, et al. Safety, Pharmacokinetics and Pharmacodynamics of the Selective Glucocorticoid Receptor Modulator AZD5423 after Inhalation in Healthy Volunteers. Basic Clin Pharmacol Toxicol. 2016 Dec;119(6):574-581.

[2]. Gauvreau GM, et al. A nonsteroidal glucocorticoid receptor agonist inhibits allergen-induced late asthmatic responses. Am J Respir Crit Care Med. 2015 Jan 15;191(2):161-7.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
573.8±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H21F4N3O3

[ Molecular Weight ]:
487.45

[ Flash Point ]:
300.8±30.1 °C

[ Exact Mass ]:
487.151917

[ PSA ]:
68.87000

[ LogP ]:
5.89

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.574

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds