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10
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13932 |
TLR1
N-[(1S)-2-甲基-1-(1-吡咯烷羰基)丙基]-苯丙酰胺 |
Others; MyD88 | Immunology/Inflammation; Others |
TLR1 是细胞穿透 Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop 的小分子模拟物,能够阻碍 IL-1 受体介导的反应。 | |||
T8503 |
TLR4-IN-C34
|
TLR | Immunology/Inflammation |
TLR4-IN-C34 是 TLR4 的抑制剂,可减少内毒素血症和坏死性小肠结肠炎模型中的全身炎症 | |||
T39669 |
TLR7/8/9-IN-1
TLR7/8/9-IN-1 |
TLR | Immunology/Inflammation |
TLR7/8/9-IN-1 是具有口服活性的Toll 样受体7/8/9小分子拮抗剂,IC50为43 nM。 | |||
T13167 |
TLR7/8 agonist 3
|
TLR | Immunology/Inflammation |
TLR7/8 agonist 3 是TLR7/8激动剂。 | |||
T7672 |
MD2-TLR4-IN-1
|
TLR | Immunology/Inflammation |
MD2-TLR4-IN-1 是一种骨髓分化蛋白 2/toll 样受体 4 (MD2-TLR4) 复合物抑制剂,能够抑制巨噬细胞 LPS 诱导的 TNF-α 和 IL-6 的表达,IC50值分别为 0.89 和 0.53 μM。 | |||
T4258 |
TLR7 agonist 2
TLR7-agonist-1,TLR7-IN-1 |
TLR | Immunology/Inflammation |
TLR7 agonist 2 (TLR7-IN-1) 是选择性 Toll 样受体 7 激动剂,LEC 值为 0.4 μM。 | |||
T38078 |
TLR7/8-IN-1
TLR7/8-IN-1 |
TLR | Immunology/Inflammation |
TLR7/8-IN-1, a crystalline TLR7/TLR8 inhibitor, is a valuable compound for autoimmune disease research[1]. | |||
T5561 |
TLR7/8 agonist 1 dihydrochloride
TLR7/8 agonist-5d,二盐酸TLR7/8 agonist 1 |
TLR | Immunology/Inflammation |
TLR7/8 agonist 1 dihydrochloride (TLR7/8 agonist-5d) 是 toll 样受体TLR7/TLR8的双重激动剂。 | |||
T38614 |
TLR7 agonist 3
|
||
TLR7 agonist 3 (Compound 2), a potent activator of toll-like receptor 7 (TLR7), plays a critical role in initiating immune responses, positioning it as a promising target for immunomodulator development. | |||
T40040 | TLR8 agonist 2 hydrochloride | ||
TLR8 agonist 2 hydrochloride is a highly potent and selective agonist for human TLR8, exhibiting an EC50 of 3 nM. However, its activity towards human TLR7 is considerably weaker, with an EC50 of 33.33 μM. | |||
T40039 |
TLR8 agonist 2
TLR8 agonist 2 |
||
TLR8 agonist 2 is a highly effective and specific compound that activates TLR8, possessing an EC 50 of 3 nM in human TLR8. Notably, TLR8 agonist 2 demonstrates lower activity towards human TLR7, with an EC 50 of 33.33 μM. | |||
T7317 |
CU-CPT-9a
|
TLR | Immunology/Inflammation |
CU-CPT-9a 是TLR8特异性拮抗剂,IC50值为 0.5 nM。 | |||
T10899 |
CU-CPT17e
|
TLR | Immunology/Inflammation |
CU-CPT17e 是多Toll 样受体激动剂,可激活TLR3、TLR8和TLR9。 | |||
T22698 |
TLR3-IN-1
CU CPT 4a |
TLR | Immunology/Inflammation |
TLR3-IN-1 (CU CPT 4a) 是一种选择性的TLR3信号抑制剂,在 RAW 264.7 细胞中 IC50 为 3.44 μM。它可以抑制 TLR3/dsRNA 复合物介导的下游信号通路,并抑制全细胞中 TNF-α 和 IL-1β 的产生。 | |||
T15020 |
CU-CPT22
|
TLR | Immunology/Inflammation |
CU-CPT22 是 toll 样受体 1 和 2 蛋白复合物抑制剂,可阻断 Pam3CSK4诱导的 TLR1/2 激活,IC50值为 0.58 µM。 它与 TLR1/2 结合的合成三酰脂蛋白竞争,Ki 值为 0.41 µM。 | |||
T39969 | TLR7/8 agonist 4 TFA | ||
TLR7/8 agonist 4 TFA (compound 41) is a highly potent TLR7/8 agonist that exhibits significant anti-cancer activity. | |||
T15777 |
Loxoribine
RWJ 21757,7-Allyl-8-oxoguanosine,洛索立宾 |
Influenza Virus; TLR | Immunology/Inflammation; Microbiology/Virology |
Loxoribine (RWJ 21757) 是一种鸟苷类似物,是一种口服生物可利用的选择性 Toll 样受体 (TLR) 7 激动剂。 具有抗病毒和抗肿瘤活性。它是一种新型的强效免疫刺激剂,具有较广谱的免疫生物学活性。 | |||
T9570 |
Enpatoran
|
TLR | Immunology/Inflammation |
Enpatoran (M5049) 是一种口服有效的TLR7/8选择性抑制剂,在HEK293 细胞中,IC50s 分别为 11.1 nM 和 24.1 nM。Enpatoran 可以阻断分子合成配体和天然内源性 RNA 配体。Enpatoran 在体内具有良好的药代动力学特性。Enpatoran 在先天性和适应性自身免疫阻断方面有研究的价值。 | |||
T11598 |
IAXO-102
|
TLR | Immunology/Inflammation |
IAXO-102 是一种 TLR4 拮抗剂,可负向调节 TLR4 信号传导,还可以防止实验性腹主动脉瘤的发展。它抑制 MAPK 和 p65 NF-κB 磷酸化和 TLR4 依赖性促炎蛋白的表达。 | |||
T39654 |
Afimetoran
BMS-986256 |
TLR | Immunology/Inflammation |
Afimetoran (BMS-986256) 是一种有效的toll 样受体拮抗剂,在炎症和自身免疫性疾病中有研究的价值。 | |||
T4231 |
MD2-IN-1
|
TLR | Immunology/Inflammation |
MD2-IN-1 是骨髓分化蛋白 2 (MD2) 的抑制剂,对重组人 MD2 (rhMD2) 的 KD 为 189 μM。 | |||
T16506 |
PF-4878691
3M-852A |
TLR | Immunology/Inflammation |
PF-4878691 (3M-852A) 是一种有效的选择性 Toll 样受体 7 激动剂,可将其抗病毒活性与其炎症活性解离。 | |||
T3502 |
C29
|
TLR | Immunology/Inflammation |
C29 是 Toll 样受体 2 抑制剂,可阻断 hTLR2/1 和 hTLR2/6 信号,IC50值分别为 19.7 和 37.6 μM。 | |||
T38547 |
TLR4-IN-C34-C2-COOH
TLR4-IN-C34-C2-COOH |
||
TLR4-IN-C34-C2-COO is a linker compound that incorporates TLR4 inhibitor TLR4-IN-C34. It effectively inhibits TLR4 activity in enterocytes and macrophages. Moreover, it demonstrates a notable ability to mitigate systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis. | |||
T7347 |
CU-CPT-8m
TLR8-specific antagonist |
TLR | Immunology/Inflammation |
CU-CPT-8m (TLR8-specific antagonist) 是TLR8特异性拮抗剂,IC50值为 67 nM。 | |||
T40423 |
L48H37
|
||
L48H37 is a chemically stable analog of Curcumin. It exhibits potent inhibitory properties against myeloid differentiation protein 2 (MD2), acting as a specific inhibitor. Its mechanism involves inhibiting the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is primarily utilized in sepsis and lung injury research [1]. | |||
T7860 |
SM-324405
SM 324405 |
TLR | Immunology/Inflammation |
SM-324405 是TLR7的激动剂,EC50 为 50 nM,对人和大鼠 TLR7 的 pEC50值分别为 7.3 和 6.6,可用于过敏性疾病的免疫治疗研究。 | |||
T17032 |
Telratolimod
MEDI9197,3M-052 |
TLR | Immunology/Inflammation |
Telratolimod (MEDI9197) 是TLR7/8的激动剂,具有抗肿瘤活性。 | |||
T8727 |
TH1020
|
TLR; Antibacterial | Immunology/Inflammation; Microbiology/Virology |
TH1020 是一种选择性 Toll 样受体 5 /鞭毛蛋白复合拮抗剂,IC50为 0.85 μM。它抑制鞭毛蛋白诱导的TLR5信号传导。 | |||
T38423 |
CL097
CL097 |
Reactive Oxygen Species; TLR | Immunology/Inflammation; Metabolism; NF-κB |
CL097 是 TLR7 和 TLR8 的有效激动剂。 CL097 诱导巨噬细胞中的促炎细胞因子和 NADPH 氧化酶引发,从而增加 fMLF 刺激的 ROS 产生。 | |||
T15371 |
Gardiquimod
|
TLR; HIV Protease | Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
Gardiquimod 可抑制巨噬细胞和活化的外周血单个核细胞的HIV-1感染。 它是一种咪唑喹啉类似物,是一种 TLR7/8 激动剂。 | |||
T5521 |
Bropirimine
U-54461,溴匹立明 |
TLR | Immunology/Inflammation |
Bropirimine (U-54461) 是 toll 样受体 7(TLR7)的合成激动剂,可通过 TLR7 介导 IFN-β 的产生抑制破骨细胞前体细胞向破骨细胞分化。它是一种生物反应调节剂,通过诱导淋巴因子起作用,在膀胱和上尿路的原位移行细胞癌中具有抗癌活性。 | |||
T23171 |
Polyinosinic-polycytidylic acid
Poly(I:C),聚胞苷酸 |
TLR | Immunology/Inflammation |
Polyinosinic-polycytidylic acid (Poly(I:C)) 是一种双链 RNA (dsRNA),是一种 TLR3 激动剂。Polyinosinic-polycytidylic acid 可以诱导哺乳动物天然免疫。 | |||
T15017 |
CU-T12-9
|
TLR | Immunology/Inflammation |
CU-T12-9 是特异性 TLR1/2激动剂,可激活先天免疫系统和适应性免疫系统。它选择性激活 TLR1/2 异二聚体,可通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号,引起下游 TNF-α、IL-10 和 iNOS 增加。 | |||
T6898 |
Motolimod
VTX-378,VTX-2337 |
TLR | Immunology/Inflammation |
Motolimod (VTX-378) 是一种有效且特异性的 Toll 样受体 8 (TLR8) 激动剂,EC50约为 100 nM。 | |||
T9765 |
TJ-M2010-5
|
MyD88 | Immunology/Inflammation |
TJ-M2010-5 是一种 MyD88 抑制剂,可与 TIR 结构域结合以干扰其同源二聚化并抑制 MyD88 信号传导。 TJ-M2010-5 可用于心肌缺血/再灌注损伤研究。 | |||
T8316 |
1V209
TLR7 agonist T7 |
TLR | Immunology/Inflammation |
1V209 (TLR7 agonist T7) 是一种 Toll 样受体 7 (TLR7) 激动剂,可与各种多糖缀合,以改善其水溶性,增强功效并保持低毒性,具有抗肿瘤作用。 | |||
T39968 |
TLR7/8 agonist 4 hydroxy-PEG10-acid
TLR7/8 agonist 4 hydroxy-PEG10-acid |
||
TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugate employed in antibody-drug conjugates (ADC). This compound exhibits remarkable antitumor activity by utilizing TLR7/8 agonist 4, which acts as a potent activator of TLR7/8. The TLR7/8 agonist 4 is linked to hydroxy-PEG10-acid, the ADC linker, via a cleavable bond. Overall, it demonstrates promising pharmaceutical potential in the context of ADC-based therapeutics. | |||
T12933 |
SM-276001
|
TLR; COX | Immunology/Inflammation; Neuroscience |
SM-276001 是可口服的干扰素诱导剂,是选择性TLR7激动剂,可以诱导抗肿瘤免疫反应。 | |||
T7302 |
CU-CPT9b
CU-CPT-9b,TLR8-specific antagonist 1 |
TLR | Immunology/Inflammation |
CU-CPT9b (TLR8-specific antagonist 1) 是 toll 样受体 8 (TLR8) 的拮抗剂,Kd 为 21 nM。它抑制由 TLR8 激动剂 R-848 在过表达 TLR8 的 HEK-Blue 细胞中诱导的 NF-ĸB 活化,IC50 值为 0.7 nM。 | |||
T6964 |
Resiquimod
R848,雷西莫特,S28463 |
HCV Protease; TLR | Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
Resiquimod (R848) 是一种 Toll 样受体7/8的激动剂,可诱导细胞因子上调。 | |||
T6846 |
Vesatolimod
GS-9620,维沙莫德 |
Apoptosis; HCV Protease; HBV; TLR; HIV Protease | Apoptosis; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
Vesatolimod (GS-9620) 是一种选择性 Toll 样受体 7 口服激动剂,EC50值为291 nM。 | |||
T9287 |
Hydroxychloroquine
2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol,羟氯喹 |
SARS-CoV; TLR; Parasite; Autophagy | Autophagy; Immunology/Inflammation; Microbiology/Virology |
Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) 是一种合成抗疟疾剂,有效抑制SARS-CoV-2感染,也抑制 Toll 样受体 7/9 信号传导。 | |||
T39970 |
TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride
TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride |
||
TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate used in antibody-drug conjugates (ADCs) with high efficacy against tumors. It consists of TLR7/8 agonist 4, a potent TLR7/8 agonist, linked to the ADC linker hydroxy-PEG10-acid which can be cleaved. | |||
T0951 |
Hydroxychloroquine sulfate
Acidum iopanoicum,硫酸羟基氯喹,硫酸羟氯喹,HCQ sulfate |
DNA; SARS-CoV; TLR; Parasite; Autophagy | Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Microbiology/Virology |
Hydroxychloroquine sulfate (Acidum iopanoicum) 抑制疟原虫血红素聚合酶。它还可抑制 Toll 样受体 7/9 信号传导和 SARS-CoV-2 感染。 | |||
T19675 |
SM360320
CL-087,SM 360320,CL 087,1V136,SM-360320,CL087 |
TLR | Immunology/Inflammation |
SM360320 (CL-087) 是一种有效的特异性 TLR7 激动剂。 SM360320 除了其 IFN 介导的活性外,还通过 I 型 IFN 非依赖性机制抑制肝细胞中的 HCV 复制。 SM360320 可用于研究作为治疗性 DNA 疫苗的免疫佐剂。 | |||
T13168 | TLR7 agonist 1 | TLR | Immunology/Inflammation |
TLR7 agonist 1 is a selective and oral TLR7 agonist (IC50: 90 nM). | |||
T12516 |
Polyinosinic-polycytidylic acid sodium
双链聚肌胞,Poly(I:C) sodium |
Apoptosis; Others; TLR | Apoptosis; Immunology/Inflammation; Others |
Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) 是双链 RNA 的合成类似物,是TLR3和视黄酸诱导型基因 I 受体激动剂。它可以用作疫苗佐剂,直接触发癌细胞发生凋亡,还增强先天性和适应性免疫反应,并改变肿瘤的微环境。 | |||
T70905 |
TLR9-IN-18
|
||
TLR9-IN-18 is a potent and selective TLR9 antagonist. TLR9-IN-18 suppresses the production of the proinflammatory cytokine IL-6 in a CpG-induced mouse model. | |||
TQ0181 |
Resatorvid
CLI-095,TAK-242,瑞沙托维 |
TNF; TLR; Autophagy; Interleukin | Apoptosis; Autophagy; Immunology/Inflammation |
Resatorvid (TAK-242) 是一种 Toll 样受体 4 (TLR4) 的抑制剂,具有选择性。Resatorvid 直接与 Cys747 结合,阻止 TLR4 与 TIRAP 结合,从而阻止下游信号转导。Resatorvid 具有抗肿瘤活性、抗炎活性和神经保护作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2S0265 |
Robinin
NSC 9222,刺槐素 |
TLR | Immunology/Inflammation |
Flavone glycoside from Robinia with antibacterial and diuretic properties; derived from kaempferol.The ability of robinin to reverse the multidrug resistance of the human colon cancer cell line Colo 320 expreβing MDR1/LRP was explored by monitoring their uptake of Rhodamine 123, but was shown to have minimal effect. Robinin (NSC-9222) was detected in lysates of the human breast cancer cell line MCF-7 using liquid chromatography-tandem maβ spectrometry. | |||
TN2008 |
Okanin
|
NF-κB; TLR | Immunology/Inflammation; NF-κB |
Okanin 是鬼针草中的一种有效成分,可通过抑制TLR4/NF-κB 信号通路减弱 LPS 诱导的小胶质细胞活化。 | |||
TQ0205 |
Procyanidin B1
原花青素B1,原花青素 B1 |
TLR | Immunology/Inflammation |
Procyanidin B1 是水果中常见的多酚类黄酮,能够与TLR4/MD-2复合体结合,具有抗炎活性。 | |||
T8689 |
Chloroquine
CQ,氯喹 |
SARS-CoV; TLR; HIV Protease; Antibiotic; Parasite; Autophagy | Autophagy; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
Chloroquine 是一种 Toll 样受体抑制剂,可以抑制自噬。Chloroquine 具有抗疟疾和抗炎活性,广泛用于治疗疟疾和类风湿性关节炎。Chloroquine 还具有抗 SARS-CoV-2 (COVID-19) 活性、抗 HIV-1 活性。 | |||
T5S0167 |
Atractylenolide I
白术内酯 I,白术内酯I;苍术内酯I |
IL Receptor; TNF; TLR; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Stem Cells |
Atractylenolide I 是从白术根中得到的一种倍半萜烯,具有神经保护、抗过敏、抗炎和抗癌等多种生物活性。它是一种TLR4拮抗剂,在 A375 细胞中,能够降低JAK2和STAT3的磷酸化水平。 | |||
T3826 |
Polygalasaponin F
异牡荆苷,瓜子金皂苷己 |
NF-κB; TLR; Akt; PI3K | Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; PI3K/Akt/mTOR signaling |
Polygalasaponin F 是从瓜子金中提取的齐墩果烷型三萜皂苷,可通过调节TLR4-PI3K/AKT-NF-kB 信号通路减少神经炎症细胞因子的分泌,能降低炎性细胞因子肿瘤坏死因子 α 的释放。 | |||
T3898 |
Schaftoside
夏佛塔苷,APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE,Shaftoside |
Dynamin; Antioxidant; TLR; MyD88; Mitochondrial Metabolism; Autophagy | Autophagy; Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; oxidation-reduction |
Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) 是在多种中草药中发现的一种黄酮类天然产物。它抑制 TLR4 和 Myd88 表达,还降低 Drp1 表达和磷酸化,并减少线粒体分裂,具有抗氧化和抗癌活性。 | |||
T5S0045 |
Isofraxidin
6,8-Dimethoxyumbelliferone,异秦皮啶,Phytodolor,异嗪皮啶 |
MMP; ERK; p38 MAPK; TLR; COX | Immunology/Inflammation; MAPK; Neuroscience; Proteases/Proteasome |
Isofraxidin (Phytodolor) 是来自刺五加的香豆素成分,抑制MMP-7表达和人肝癌细胞侵袭。它作用于肝癌细胞,抑制ERK1/2磷酸化。它减弱iNOS 和COX-2表达,还抑制TLR4/髓样分化蛋白 2 复合物的形成。 | |||
T0194 |
Chloroquine phosphate
Chloroquine diphosphate,Aralen phosphate,磷酸氯喹,Chingamin phosphate |
SARS-CoV; TLR; HIV Protease; Antibiotic; Parasite; Autophagy | Autophagy; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
Chloroquine phosphate (Aralen phosphate) 是广泛用于疟疾和类风湿性关节炎的抗疟疾和抗炎剂。它是autophagy 和toll-like receptors 抑制剂,有效抑制SARS-CoV-2(COVID-19) 感染 (EC50=1.13 μM)。 | |||
T6S1487 |
Ginsenoside Rg5
人参皂苷Rg5,人参皂甙 Rg5 |
NF-κB; COX; IGF-1R | Immunology/Inflammation; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors |
Ginsenoside Rg5 是红参的主要成分,可阻断IGF-1与其受体的结合,IC50约为90 nM。它还通过抑制NF-κB p65的 DNA 结合活性来抑制COX-2的 mRNA 表达。它可促进血管生成和改善高血压,具有抗炎和治疗阿尔茨海默病的潜力。 |