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Al-438

Names

[ CAS No. ]:
239066-73-0

[ Name ]:
Al-438

Biological Activity

[Description]:

AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity[1][2].

[Related Catalog]:

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

[Target]

Ki: 2.5 nM (glucocorticoid receptor)[1]


[In Vitro]

AL-438 (1 µM) 降低 ATDC5 细胞中 LPS 诱导的 IL-6 的生成[1]。 AL-438 (0-1 µM; 1 h+24 h) 抑制 HSKF1501 细胞中 IL-1β (2 ng/ml) 诱导的 IL-6 表达[2]。

[In Vivo]

AL-438 (1, 10, 100 mg/kg; p.o.) 在大鼠体内显示出抗炎活性[2]。 Animal Model: Male Sprague Dawley rats (carrageenan paw edema model)[2] Dosage: 1, 10, 100 mg/kg Administration: P.o. Result: Showed antiinflammatory activity with ED50 value of 11 mg/kg in acute inflammation assay.

[References]

[1]. Owen HC, et al. The growth plate sparing effects of the selective glucocorticoid receptor modulator, AL-438. Mol Cell Endocrinol. 2007 Jan 29;264(1-2):164-70.  

[2]. Coghlan MJ, et al. A novel antiinflammatory maintains glucocorticoid efficacy with reduced side effects. Mol Endocrinol. 2003 May;17(5):860-9.  

Chemical & Physical Properties

[ Molecular Formula ]:
C23H25NO2

[ Molecular Weight ]:
347.45

Related Compounds