2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. Toll-like Receptor (TLR) Stearoyl-CoA Desaturase (SCD)
  4. E6446 dihydrochloride

E6446 dihydrochloride 

目录号: HY-12756A 纯度: 99.96%
COA 产品使用指南

摩尔计算器

E6446 dihydrochloride 是一种有效的、可口服的 TLR7 和 TLR9 拮抗剂，可用于有害炎症反应的研究。E6446 dihydrochloride 还是强效的 SCD1 抑制剂 (KD: 4.61 μM)，通过 SCD1-ATF3 信号传导显着抑制脂肪形成分化和肝脂肪生成。E6446 dihydrochloride 还改善高脂饮食 (HFD) 喂养小鼠的肝脏病变，可用于非酒精性脂肪肝病 (NAFLD) 的研究。

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E6446 dihydrochloride Chemical Structure

E6446 dihydrochloride Chemical Structure

CAS No. : 1345675-25-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2874
In-stock
1 mg ￥1136
In-stock
5 mg ￥2500
In-stock
10 mg ￥3900
In-stock
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100 mg   询价  

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Customer Review

Other Forms of E6446 dihydrochloride:

E6446 dihydrochloride 相关抗体

Top Publications Citing Use of Products

查看 Toll-like Receptor (TLR) 亚型特异性产品:

查看所有亚型
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

E6446 dihydrochloride is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 dihydrochloride is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 dihydrochloride also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD)[1][2][3].

IC50 & Target[1][3]

TLR7

 

TLR9

 

体外研究
(In Vitro)

E6446 dihydrochloride 是一种有效的口服活性 TLR7 和 TLR9 抑制剂。E6446 dihydrochloride 有效抑制 HEK:TLR9 细胞的 DNA 刺激，IC50 值为 10 nM，但在抑制 HEK:TLR4 细胞的 LPS 内毒素刺激或 HEK:TLR7 细胞的 R848 刺激方面效果明显较差. E6446 dihydrochloride 有效抑制 CpG2216 诱导的 IL-6 产生，但对 TLR3 配体聚肌苷-胞嘧啶的诱导无效。E6446 dihydrochloride 抑制 TLR7 的能力是配体依赖性的，E6446 dihydrochloride 是 RNA 诱导 IL-6 的有效抑制剂，但对小分子咪唑喹啉配体 R-848 诱导 IL-6 的抑制剂相对较弱。E6446 dihydrochloride 在体外抑制 TLR9-DNA 相互作用，IC50 在 1 到 10 μM 范围内[1]。E6446 dihydrochloride (0.01-0.03 μM) 用 CpG ODN 2006 特异性抑制 TLR9 激活，并在 2-8 μM 时阻断由咪唑喹啉化合物 R848 激活的 TLR7/8。E6446 dihydrochloride 在 30 μM 时减少 50% 的 TLR4 激活，并且在用 oligo 2006 刺激的 HEK-TLR9 细胞和用 oligo 2216 刺激的人 PBMC 中显示 IC50 分别为 0.01 μM 和 0.23 μM[2]。

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

E6446 dihydrochloride 相关抗体:
体内研究
(In Vivo)

E6446 dihydrochloride (20 mg/kg，口服) 几乎完全抑制 CpG1668 诱导的 IL-6 产生，并在 20 和 60 mg/kg 剂量依赖性地抑制小鼠体内 ANA (抗核抗体) 的产生[1]。E6446 dihydrochloride (20，60 mg/kg，po) 剂量依赖性地抑制小鼠中的 TLR9 信号传导。E6446 dihydrochloride (60、120 mg/kg，口服) 可防止啮齿动物疟疾中 TLR 的高反应性和 LPS 诱导的感染性休克，降低急性疟疾期间的 TLR 反应性，抑制 TLR7 和 TLR9 的激活[2]。

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

522.51

Formula

C27H37Cl2N3O3
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 7.6 mg/mL (14.55 mM; 超声加热助溶; 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 1.9138 mL 9.5692 mL 19.1384 mL
5 mM 0.3828 mL 1.9138 mL 3.8277 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

只
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: 99.96%

COA (188 KB) HNMR (150 KB) LCMS (339 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

E6446 is assayed for the suppression of BALB/c mouse spleen interleukin-6 (IL-6) production in response to stimulation by oligonucleotide CpG1668. E6446 is added to dissociated splenocytes (5 × 105 per well in complete RPMI/10% fetal bovine serum in a 96-well plate) before addition of TLR agonists. Cells are stimulated for 72 hours, and supernatants are removed for ELISA analysis of IL-6. Mouse bone marrow-derived dendritic cells (BMDCs) are generated by culturing BALB/c marrow cells in RPMI containing 100 ng/mL Flt3 ligand for 7 days. Cells (1 × 105) in 50 μL are assayed for IL-6 production after overnight or 24-hour stimulation with various TLR ligands. For studies using human peripheral blood mononuclear cells, Ficoll-separated mononuclear cells are isolated from healthy volunteer donors, washed, and plated with stimulatory oligonucleotide CpG2216 in complete RPMI for 72 hours. Interferon in supernatant is quantified by ELISA[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
MRL/lpr mice are dosed orally five times a week with 20 or 60 mg/kg E6446 or 60 mg/kg hydroxychloroquine beginning at 5 weeks of age. Cytoxan is administered at 50 mg/kg i.p. every 10 days. A serum sample is taken immediately before the beginning of treatment to monitor changes in autoreactive antibodies. Subsequently, serum samples are collected approximately monthly and analyzed for anti-dsDNA by ELISA after 1:500 dilution. Body weights and urine samples are taken at the same interval, and proteinuria is assessed by ChemStrips. Anti-nuclear antibodies (ANA) are assessed using commercially available HEp2 slide kits, with serum diluted to 1:100 in kit buffer. ANA scores are read blinded[1].

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

E6446 dihydrochloride 相关分类

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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9138 mL 9.5692 mL 19.1384 mL 47.8460 mL
5 mM 0.3828 mL 1.9138 mL 3.8277 mL 9.5692 mL
10 mM 0.1914 mL 0.9569 mL 1.9138 mL 4.7846 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.

Keywords:

E64461345675-25-3E 6446E-6446Toll-like Receptor (TLR)Stearoyl-CoA Desaturase (SCD)high-fat dietnon-alcoholic fatty liver diseaseNAFLDadipogenic differentiationhepatic lipogenesisInhibitorinhibitorinhibit

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