TH 1020 |
カタログ番号GC50374
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TH 1020はToll様の受容体5（TLR5）/フラジェリン複合体の拮抗剤であり、IC50値は0.85μMである。
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Cas No.: 1841460-82-9
Sample solution is provided at 25 µL, 10mM.
TH 1020はToll様の受容体5（TLR5）/フラジェリン複合体の拮抗剤であり、IC50値は0.85μMである[1]。TH 1020はフラジェリン誘発のTLR5のシグナル伝達を阻害できるが、TLR2、TLR3、TLR4、TLR7とTLR8に対しては無効である[2]。TH 1020は、TLR5二量体の間の分子インターフェースと結合することで、下流シグナル伝達を阻害し、機能性四量体複合体の機能を抑制する[3]。TH 1020は、CD8+ T細胞で、TLR5シグナル伝達を阻害できる[4]。
体外で、腸管毒素原性大腸菌（ETEC）C83901株に感染したIPEC-J2細胞をTH 1020 (1.5μM)で2時間事前処理した結果、細胞内IL-17Cの分泌を完全に阻害した[5]。TH 1020 (0.75, 1.5μM)で一次末梢血単核細胞（PBMC）を処理した結果、フラジェリンと高移動性グループのタンパク質B1（HMGB1）が誘発した一酸化窒素（NO）の産生を著しく減らした[6]。
体内で、卵巣癌モデルマウスにTH 1020 (100μg)を4日間腹腔内注射した結果、腫瘍微小環境で、CCR2+ Ly6C+細胞の数と腫瘍浸潤マクロファージの総数を著しく減らした[7]。
References:
[1] Patra M C, Choi S. Recent progress in the development of Toll-like receptor (TLR) antagonists[J]. Expert opinion on therapeutic patents, 2016, 26(6): 719-730.
[2] Yan L, Liang J, Yao C, et al. Pyrimidine triazole thioether derivatives as Toll‐like receptor 5 (TLR5)/flagellin complex inhibitors[J]. ChemMedChem, 2016, 11(8): 822-826.
[3] Leifer C A, Medvedev A E. Molecular mechanisms of regulation of Toll-like receptor signaling[J]. Journal of Leucocyte Biology, 2016, 100(5): 927-941.
[4] Kang X, Liu C, Ding Y, et al. Roseburia intestinalis generated butyrate boosts anti-PD-1 efficacy in colorectal cancer by activating cytotoxic CD8+ T cells[J]. Gut, 2023, 72(11): 2112-2122.
[5] Luo Y, Xu J, Zhang C, et al. Toll-like receptor 5-mediated IL-17C expression in intestinal epithelial cells enhances epithelial host defense against F4+ ETEC infection[J]. Veterinary research, 2019, 50(1): 48.
[6] Das N, Dewan V, Grace P M, et al. HMGB1 activates proinflammatory signaling via TLR5 leading to allodynia[J]. Cell reports, 2016, 17(4): 1128-1140.
[7] Kolli S H, McGinty M T, Putelo A M, et al. Ovarian Cancer Drives TLR5-Dependent Expansion of Myeloid Progenitors Through Systemic Dissemination of Ligands[J]. bioRxiv, 2025: 2025.06. 10.658497.
| 細胞実験[1]: | |
細胞株 | IPEC-J2単層 |
準備方法 | まず、IPEC-J2単層を0.5μMのTH 1020 (0.5μM)、0.5μMのオリゴデオキシリボヌクレオチド(ODN) 2088または等量の溶媒DMSOとTEまたはPBSで2時間事前培養した。次に、単層に、MOI 100で、C83901 (腸管毒素原性大腸菌（ETEC）参照株)を1時間接種し、洗浄し、更に23時間インキュベートした。細胞培養上清で、IL-17Cサイトカインの産生をELISAで分析した。 |
反応条件 | 0.5μM；2時間 |
アプリケーション | C83901感染のIPEC-J2細胞で、TH 1020はIL-17Cの分泌をほぼ完全に阻害した。 |
References: | |
| Cas No. | 1841460-82-9 | SDF | |
| Canonical SMILES | N1(C(SC2=C3SC4=NC=CC=C4C3=NC=N2)=NN=C1C5=CC=NC=C5)CC6=CC=CC=C6 | ||
| Formula | C23H15N7S2 | M.Wt | 453.54 |
| 溶解度 | Chloroform: 1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2049 mL | 11.0244 mL | 22.0488 mL |
| 5 mM | 441 μL | 2.2049 mL | 4.4098 mL |
| 10 mM | 220.5 μL | 1.1024 mL | 2.2049 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)