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Glucocorticoid receptor modulator 1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Glucocorticoid receptor modulator 1图片
CAS NO:2868357-11-1
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Glucocorticoid receptor modulator 1 是一种高效且具有口服活性的NF-κB和AP-1抑制剂，IC50分别为 9 nM 和 130 nM。Glucocorticoid receptor modulator 1 可有效降低炎症因子 IL-6、IL-1β、TNF-α 的表达，可缓解小鼠皮炎。
生物活性

Glucocorticoid receptor modulator1 is a highly potent and orally active non-steroidal selectiveglucocorticoid receptormodulator with anIC50value of 9 nM and 130 nM forNF-κBandAP-1, respectively.Glucocorticoid receptor modulator1 can effectively reduce the expression of inflammatory factorsIL-6, IL-1β, TNF-α, also can relieve dermatitis in mice[1].

IC50& Target

IC50: 9 nM (NF-κB), 130 nM (AP-1)[1]

体外研究
(In Vitro)

Glucocorticoid receptor modulator 1 (compound B53) shows inhibitory activities against NF-κB and AP-1 with IC50s of 9 nM and 130 nM, respectively[1].
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[1].

RT-PCR[1]

Cell 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 IC50s of 6.90 μM and 7.74 μM, respectively.
体内研究
(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[1].

Animal Model:Female BALB/C mice (5 weeks; 2,4-dinitrochlorobenzene-induced atopic dermatitis model)[1]
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.
分子量

470.97

Formula

C24H23ClN2O4S

CAS 号

2868357-11-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.