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Glucocorticoid receptor modulator 1

目录号 : GC71181

Glucocorticoid receptor modulator 1是一种口服活性非甾体选择性糖皮质激素受体调节剂,对NF-κB和AP-1的IC50值分别为9 nM和130 nM。

Glucocorticoid receptor modulator 1 Chemical Structure

Cas No.:2868357-11-1

规格 价格 库存 购买数量
1 mg
¥1,309.00
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5 mg
¥2,880.00
现货
10 mg
¥4,590.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 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.

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].

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].

References:
[1]. Li D, Hou T, et al. Discovery and Optimization of N-Acyl-6-sulfonamide-tetrahydroquinoline Derivatives as Novel Non-Steroidal Selective Glucocorticoid Receptor Modulators. J Med Chem. 2022 Nov 18.

Chemical Properties

Cas No. 2868357-11-1 SDF
分子式 C24H23ClN2O4S 分子量 470.97
溶解度 DMSO : 100 mg/mL (212.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 4°C, sealed storage, away from moisture and light
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1 mg 5 mg 10 mg
1 mM 2.1233 mL 10.6164 mL 21.2328 mL
5 mM 0.4247 mL 2.1233 mL 4.2466 mL
10 mM 0.2123 mL 1.0616 mL 2.1233 mL
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