1. NF-κB
  2. NF-κB
  3. Bezisterim

Bezisterim  (Synonyms: HE 3286; NE-3107)

目录号: HY-108039 纯度: ≥95.0%
COA 产品使用指南

Bezisterim (HE 3286; NE-3107) 是天然抗炎类固醇 β-AET 的合成衍生物。Bezisterim 是具有口服活性的 NF-κB 部分抑制剂。Bezisterim 降低了促炎信号,包括 IL-6 和基质金属肽酶 3。Bezisterim 可自由穿过小鼠血脑屏障。Bezisterim 可用于溃疡性结肠炎、关节炎、实验性自身免疫性脑脊髓炎的研究。Bezisterim 是一种点击化学试剂。它含有 Alkyne 基团,可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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Bezisterim Chemical Structure

Bezisterim Chemical Structure

CAS No. : 1001100-69-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3300
In-stock
1 mg ¥1363
In-stock
5 mg ¥3000
In-stock
10 mg ¥4800
In-stock
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

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

Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis[1][2][3]. Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

NF-κB[3]

体外研究
(In Vitro)

Bezisterim attenuates NF-κB phosphorylation, but not influences IκB phosphorylation of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages[3].
Bezisterim (100 nM, overnight) partially blocks the activation of IKK, JNK, p38, and ERK of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages[3].

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

Western Blot Analysis[3]

Cell Line: LPS-induced murine macrophages
Concentration: 100 nM
Incubation Time: overnight
Result: Attenuated NF-κB phosphorylation.
Blocked the activation of IKK, JNK, p38, and ERK partially.
体内研究
(In Vivo)

Bezisterim (25-50 mg/kg; oral gavage; daily for 22-49 days) reduces joint inflammation, synovial proliferation, and erosion of DBA/1 Lac male collagen-induced arthritis mice [1].
Bezisterim (40 mg/kg; intraperitoneal injection; daily for 40 days) suppresses inflammation, reduces demyelination and axonal loss, and promotes RGC survival during experimental optic neuritis of experimental autoimmune encephalomyelitis mice[2].
Bezisterim (80?mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice[4].
Bezisterim (40 mg/kg; gavage; twice-daily for 4 days) increases the numbers of tyrosine hydroxylase-positive cells and decreases the numbers of damaged neurons in Parkinson's disease mice[4].

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

Clinical Trial
分子量

330.46

Formula

C21H30O3

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (302.61 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 3.0261 mL 15.1304 mL 30.2609 mL
5 mM 0.6052 mL 3.0261 mL 6.0522 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)。-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

纯度: ≥95.0%

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)。-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 3.0261 mL 15.1304 mL 30.2608 mL 75.6521 mL
5 mM 0.6052 mL 3.0261 mL 6.0522 mL 15.1304 mL
10 mM 0.3026 mL 1.5130 mL 3.0261 mL 7.5652 mL
15 mM 0.2017 mL 1.0087 mL 2.0174 mL 5.0435 mL
20 mM 0.1513 mL 0.7565 mL 1.5130 mL 3.7826 mL
25 mM 0.1210 mL 0.6052 mL 1.2104 mL 3.0261 mL
30 mM 0.1009 mL 0.5043 mL 1.0087 mL 2.5217 mL
40 mM 0.0757 mL 0.3783 mL 0.7565 mL 1.8913 mL
50 mM 0.0605 mL 0.3026 mL 0.6052 mL 1.5130 mL
60 mM 0.0504 mL 0.2522 mL 0.5043 mL 1.2609 mL
80 mM 0.0378 mL 0.1891 mL 0.3783 mL 0.9457 mL
100 mM 0.0303 mL 0.1513 mL 0.3026 mL 0.7565 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:
Bezisterim
目录号:
HY-108039
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