1821387-73-8

中文名称 CU-T12-9

英文名称 CU-T12-9

CAS 1821387-73-8

分子式 C17H13F3N4O2

分子量 362.31

MOL 文件 1821387-73-8.mol

更新日期 2024/07/12 16:05:26

1821387-73-8 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物CU-T12-9

英文别名

CU-T12-9
N-methyl-4-nitro-2-[4-[4-(trifluoromethyl)phenyl]imidazol-1-yl]aniline
Benzenamine, N-methyl-4-nitro-2-[4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-

物理化学性质

沸点524.3±50.0 °C(Predicted)

密度1.39±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMSO: 250 mg/mL (690.02 mM)

酸度系数(pKa)3.53±0.10(Predicted)

形态固体

颜色Light yellow to yellow

常见问题列表

生物活性

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。

靶点

TLR2

52.9 nM (EC ₅₀ , in HEK-Blue cells)

TLR1

52.9 nM (EC ₅₀ , in HEK-Blue cells)

体外研究

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.
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.
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.
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.

Cell Cytotoxicity Assay

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

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.