标签归档：tlr

CU-T12-9

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CU-T12-9  纯度: 99.94%

CU-T12-9 是一种特异性 TLR1/2 激动剂，EC50 为 52.9 nM。CU-T12-9 既激活先天免疫系统，又激活适应性免疫系统。CU-T12-9 选择性激活 TLR1/2 异二聚体而对 TLR2/6 没有作用。CU-T12-9 通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号，致使下游 TNF-α，IL-10，和 iNOS 增加，从而提高身体的免疫反应。

CU-T12-9

CU-T12-9 Chemical Structure

CAS No. : 1821387-73-8

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10 mM * 1 mL in DMSO ￥877 In-stock
5 mg ￥1100 In-stock
10 mg ￥1800 In-stock
50 mg ￥5500 In-stock
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CU-T12-9 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Antioxidants Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library

生物活性

CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS[1].

IC50 & Target[1]

TLR2

52.9 nM (EC50, in HEK-Blue cells)

TLR1

52.9 nM (EC50, in HEK-Blue cells)

体外研究
(In Vitro)

CU-T12-9 directly targets TLR1/2 to initiate downstream signaling. By binding to both TLR1 and TLR2, CU-T12-9 facilitates the TLR1/2 heterodimeric complex formation, which in turn activates the downstream signaling[1].
CU-T12-9 activates the TLR1/2 pathway by inducing NF-κB activation to trigger downstream signaling, such as secreted embryonic alkaline phosphatase (SEAP), NO, and TNF-α[1].
CU-T12-9 (0.39-100 μM; 24 hours) does not produce toxicity up to 100 μM in HEK-Blue hTLR2 and Raw 264.7 cells[1].
CU-T12-9 up-regulates the mRNA levels of TLR1, TLR2, TNF, IL-10, and iNOS. CU-T12-9 (0.1-10 μM) activates TLR1 mRNA and iNOS mRNA after Raw 264.7 cells are treated for 24 hours. CU-T12-9 (0.1-10 μM) activates TLR2 and IL-10 mRNA after Raw 264.7 cells are treated for 2 hours. CU-T12-9 (0.1-10 μM) activates TNF mRNA after Raw 264.7 cells are treated for 8 hours[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: HEK-Blue hTLR2 and Raw 264.7 macrophage cells
Concentration: 0.39, 0.78, 1.56, 3.125, 6.25, 12.5, 25, 50, and 100 μM
Incubation Time: 24 hours
Result: No toxicity was seen up to 100 μM.

RT-PCR[1]

Cell Line: Raw 264.7 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 hours for TLR1 and iNOS mRNA assay
2 hours for TLR2 and IL-10 mRNA assay
8 hours for TNF mRNA assay
Result: Triggered TLR1 mRNA and iNOS mRNA at 24 hours dose-dependently.
Dose-dependent activation of TLR2 mRNA and IL-10 mRNA at 2 hours.
Showed dose-dependent activation of TNF mRNA at 8 hours.

分子量

362.31

Formula

C17H13F3N4O2
CAS 号

1821387-73-8
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (690.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7601 mL 13.8003 mL 27.6007 mL
5 mM 0.5520 mL 2.7601 mL 5.5201 mL
10 mM 0.2760 mL 1.3800 mL 2.7601 mL

*

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.74 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.74 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cheng K, et al. Specific activation of the TLR1-TLR2 heterodimer by small-molecule agonists. Sci Adv. 2015;1(3). pii: e1400139.

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TLR7/8 agonist 4 TFA

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TLR7/8 agonist 4 TFA 

TLR7/8 agonist 4 TFA (compound 41) 是一种有效的 TLR7/8 激动剂。TLR7/8 agonist 4 具有抗癌活性。

TLR7/8 agonist 4 TFA

TLR7/8 agonist 4 TFA Chemical Structure

CAS No. : 2388520-34-9

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生物活性

TLR7/8 agonist 4 TFA (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity[1].

IC50 & Target[1]

TLR7

 

TLR8

 

分子量

438.45

Formula

C20H25F3N6O2
CAS 号

2388520-34-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Shelley Erin ACKERMAN, et al. Macromolecule-supported tlr agonists. WO2020190762A1.

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TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride 

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) 是抗体-药物偶联物的一部分，由 TLR7/8 激活剂 TLR7/8 agonist 4 (HY-139018) 和可降解的 ADC linker hydroxy-PEG10-acid (HY-133307) 连接而成。

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride Chemical Structure

CAS No. : 2388520-36-1

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the cleavable ADC linker hydroxy-PEG10-acid (HY-133307)[1].

IC50 & Target[1]

Traditional Cytotoxic Agents

 

体外研究
(In Vitro)

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

873.47

Formula

C41H69ClN6O12
CAS 号

2388520-36-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Shelley Erin ACKERMAN, et al. Immunoconjugates targeting her2. WO2020190725A1.

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