Glucocorticoid receptor modulator 1

Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC 50 value of 9 nM and 130 nM for NF-κB and AP-1 , respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6 , IL-1β, TNF-α, also can relieve dermatitis in mice In Vitro Glucocorticoid receptor modulator 1 (compound B53) shows inhibitory activities against NF-κB and AP-1 with IC 50 s of 9 nM and 130 nM, respectively. Glucocorticoid receptor modulator 1 (10 μM; 24 h) decreases the mRNA expression of the inflammatory factors of IL-6, IL-1β, TSLP, MMP-13, TNF-α, and CCL-2. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: Mouse macrophage RAW264.7 cells Concentration: 10 μM Incubation Time: 24 h Result: Practically decreased the mRNA expression of the inflammatory factors of IL-6, IL-1β, TSLP, MMP-13, TNF-α, and CCL-2. Reduced IL-6 and TNF-α dose-dependently with IC 50 s of 6.90 μM and 7.74 μM, respectively. In Vivo Glucocorticoid receptor modulator 1 (5, 10 and 20 mg/kg; p.o.; for 24 days) relieves dermatitis in mice and suppresses the expression of inflammatory factors . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/C mice (5 weeks; 2,4-dinitrochlorobenzene-induced atopic dermatitis model) Dosage: 5, 10 and 20 mg/kg Administration: p.o.; for 24 days Result: Significantly improved the skin damage in a dose-dependent manner, and suppressed inflammatory factors of IL-6, IL-1β, TSLP, and MMP-13. Form:Solid IC50& Target:IC 50 : 9 nM (NF-κB), 130 nM (AP-1)

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