1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. TLR7 agonist 2

TLR7 agonist 2 是一种有效且有选择性的 Toll 样受体 7 (TLR7) 激动剂,LEC 值为 0.4 μM。

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TLR7 agonist 2 Chemical Structure

TLR7 agonist 2 Chemical Structure

CAS No. : 1642857-69-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3330
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1 mg ¥1500
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5 mg ¥4488
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10 mg ¥6082
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25 mg ¥9732
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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Toll-like Receptor (TLR) 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

IC50 & Target

LEC: 0.4 μM (TLR7)[1]

体外研究
(In Vitro)

TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a lowest effective concentration (LEC) of 0.4 μM in HEK293 cell. TLR7 agonist 2 is found to be selective for TLR7 over TLR8 with LEC of >100 μM for human TLR8. TLR7 agonist 2 demonstrates low inhibition across five CYP450 isozymes (IC50 >10 μM) and is also not a time dependent inhibitor of CYP450 3A4. TLR7 agonist 2 has limited inhibition of the hERG potassium ion channel 3H-dofetilide binding in vitro (IC50 >50 μM)[1].

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

体内研究
(In Vivo)

TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both Cmax and AUC increase less than dose proportionally between 0.3 and 3 mg/kg and more than dose-proportionally between 3 and 10 mg/kg. TLR7 agonist 2 can induce an antiviral interferon stimulated gene (ISG) response without inducing an IFNα response at a low dose. TLR7 agonist 2 also induces a 2.7 log decrease in serum HBV viral load from 0.3 mg/kg, and a maximum 3.1 log decrease is observed for doses between 1 and 5 mg/kg[1].

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

分子量

336.35

Formula

C17H16N6O2

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
细胞实验: 

DMSO 中的溶解度 : 160 mg/mL (475.69 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 2.9731 mL 14.8655 mL 29.7309 mL
5 mM 0.5946 mL 2.9731 mL 5.9462 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

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
Cell Assay
[1]

The ability of TLR7 agonist 2 to activate human TLR7 and/or TLR8 is assessed by using HEK293 cells. Briefly, HEK293 cells are grown in culture medium (DMEM supplemented with 10% FCS and 2 mM Glutamine). Transfected cells are then detached with Trypsin-EDTA, washed in PBS and resuspended in medium to a density of 1.67×105 cells/mL. Thirty microliters of cells are then dispensed into each well in 384-well plates, where 10 μL of TLR7-agonist-1 in 4% DMSO is already present. Following 6 hours incubation at 37°C, 5% CO2, the luciferase activity is determined by adding 15 μL of Steady Lite Plus substrate to each well and readout performed on a microplate imager. Lowest effective concentrations (LEC) values are determined for TLR7-agonist-1[1].

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

Animal Administration
[1]

A mouse in vivo model is used to demonstrate the initial proof of concept to induce endogenous IFNα. Single oral administration of 0.3, 1, 3, and 10 mg/kg doses of TLR7 agonist 2 is given to healthy, female, fasted C57Bl/6 mice. Concentrations of TLR7 agonist 2 and mouse-IFN via ELISA are measured from the plasma and compare to vehicle[1].

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

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, 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 2.9731 mL 14.8655 mL 29.7309 mL 74.3273 mL
5 mM 0.5946 mL 2.9731 mL 5.9462 mL 14.8655 mL
10 mM 0.2973 mL 1.4865 mL 2.9731 mL 7.4327 mL
15 mM 0.1982 mL 0.9910 mL 1.9821 mL 4.9552 mL
20 mM 0.1487 mL 0.7433 mL 1.4865 mL 3.7164 mL
25 mM 0.1189 mL 0.5946 mL 1.1892 mL 2.9731 mL
30 mM 0.0991 mL 0.4955 mL 0.9910 mL 2.4776 mL
40 mM 0.0743 mL 0.3716 mL 0.7433 mL 1.8582 mL
50 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4865 mL
60 mM 0.0496 mL 0.2478 mL 0.4955 mL 1.2388 mL
80 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9291 mL
100 mM 0.0297 mL 0.1487 mL 0.2973 mL 0.7433 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:
TLR7 agonist 2
目录号:
HY-103039
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