1. Vitamin D Related/Nuclear Receptor NF-κB Immunology/Inflammation
  2. Glucocorticoid Receptor NF-κB AP-1
  3. Glucocorticoid receptor modulator 1

Glucocorticoid receptor modulator 1 

目录号: HY-151876 纯度: 99.79%
COA 产品使用指南

Glucocorticoid receptor modulator 1 是一种高效且具有口服活性的 NF-κBAP-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。

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Glucocorticoid receptor modulator 1 Chemical Structure

Glucocorticoid receptor modulator 1 Chemical Structure

CAS No. : 2868357-11-1

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查看 NF-κB 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

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)[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
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (212.33 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1233 mL 10.6164 mL 21.2328 mL 53.0819 mL
5 mM 0.4247 mL 2.1233 mL 4.2466 mL 10.6164 mL
10 mM 0.2123 mL 1.0616 mL 2.1233 mL 5.3082 mL
15 mM 0.1416 mL 0.7078 mL 1.4155 mL 3.5388 mL
20 mM 0.1062 mL 0.5308 mL 1.0616 mL 2.6541 mL
25 mM 0.0849 mL 0.4247 mL 0.8493 mL 2.1233 mL
30 mM 0.0708 mL 0.3539 mL 0.7078 mL 1.7694 mL
40 mM 0.0531 mL 0.2654 mL 0.5308 mL 1.3270 mL
50 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0616 mL
60 mM 0.0354 mL 0.1769 mL 0.3539 mL 0.8847 mL
80 mM 0.0265 mL 0.1327 mL 0.2654 mL 0.6635 mL
100 mM 0.0212 mL 0.1062 mL 0.2123 mL 0.5308 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Glucocorticoid receptor modulator 1
目录号:
HY-151876
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