TH 1020 |
رقم الكتالوجGC50374
One-Click Copy Product Info
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TH 1020 عبارة عن مناهض مركب قوي وانتقائي شبيه برسم المرور 5 (TLR5) / فلاجيلين مع IC50 يبلغ 0.85 ميكرومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1841460-82-9
Sample solution is provided at 25 µL, 10mM.
TH 1020 is a Toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 value of 0.85μM[1]. TH 1020 can inhibit flagellin-induced TLR5 signaling, but is ineffective against TLR2, TLR3, TLR4, TLR7, and TLR8[2]. TH 1020 inhibits downstream signaling by binding to the molecular interface between TLR5 dimers, disrupting the formation of functional tetramer complexes[3]. TH 1020 can inhibit TLR5 signaling in CD8+ T cells[4].
In vitro, pretreatment of IPEC-J2 cells infected with enterotoxigenic Escherichia coli (ETEC) strain C83901 with TH 1020 (1.5μM) for 2h completely inhibited the secretion of intracellular IL-17C[5]. Treatment of primary peripheral blood mononuclear cells (PBMCs) with TH 1020 (0.75, 1.5μM) significantly reduced the production of nitric oxide (NO) induced by flagellin and high mobility group protein B1 (HMGB1)[6].
In vivo, intraperitoneal injection of TH 1020 (100μg) for 4 days in ovarian cancer model mice significantly reduced the number of CCR2+ Ly6C+ cells in the tumor microenvironment and the total number of tumor-infiltrating macrophages[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.
| Cell experiment [1]: | |
Cell lines | IPEC-J2 monolayers |
Preparation Method | IPEC-J2 monolayers were first pre-cultured with 0.5μM TH 1020 (0.5μM), 0.5μM oligodeoxyribonucleotide (ODN) 2088 or the equivalent amount of their solvent DMSO and TE or PBS for 2h. Then, the monolayers were inoculated with the C83901 (Enterotoxigenic Escherichia coli (ETEC) reference strain) at MOI 100 for 1h, washed and further incubated for 23h. IL-17C cytokine production was analysed in the cell culture supernatant by ELISA. |
Reaction Conditions | 0.5μM; 2h |
Applications | TH 1020 almost completely inhibited the secretion of IL-17C in C83901-infected IPEC-J2 cells. |
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 |
| الذوبان | 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 DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)