TH 1020 |
Catalog No.GC50374
One-Click Copy Product Info
|
TH 1020는 IC50 0.85 μM의 TLR5/플라젤린 복합체 길항제이다.
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 1020는 IC50 0.85 μM의 TLR5/플라젤린 복합체 길항제이다. TH 1020는 플라젤린에 의해 유도되는 TLR5 신호를 억제하지만 TLR2, TLR3, TLR4, TLR7, TLR8에는 효과가 없다 [2]. TH 1020는 TLR5 이량체 분자 계면에 결합해서 기능적 사량체 복합체 형성을 파괴해서 하위 신호전달을 억제한다 [3]. TH 1020는 CD8⁺ T 세포에서 TLR5 신호 전달을 억제할 수 있다 [4].
체외 실험에서 IPEC-J2 세포를 1.5 μM TH 1020으로 2시간 전처리한 후 장독소형 대장균(ETEC) C83901주를 감염시켰을 때 세포내 IL-17C 분비가 완전하게 억제되었다 [5]. 0.75, 1.5 μM TH 1020으로 원발성 말초혈액 단핵세포(PBMCs)를 처리하면 플라젤린과 고이동성군단백 B1(HMGB1)이 공동으로 유도한 산화질소(NO) 생성이 현저하게 감소하였다 [6].
난소암 모델 쥐에게 4일간 TH 1020(100 μg)을 복강내 주입하면 종양 미세환경 내 CCR2⁺ Ly6C⁺ 세포 수와 전체 종양 침윤 대식세포 수가 현저하게 감소하였다[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.
| 세포 실험 [1]: | |
세포 라인 | IPEC-J2 단층 세포 |
제조 방법 | IPEC-J2 단층 세포를 0.5 μM TH 1020, 0.5 μM 올리고데옥시리보뉴클레오타이드(ODN) 2088 또는 동량의 용매 DMSO/TE 및 PBS로 2시간 전처리한 후 MOI 100으로 C83901(Enterotoxigenic Escherichia coli (ETEC) 참고 균주)을 1시간 감염시켰습니다. 세척 후 23시간 추가 배양하고 배양 상청액에서 ELISA로 IL-17C 사이토카인을 측정하였습니다. |
반응 조건 | 0.5μM; 2 시간 동안 |
응용 분야 | TH 1020는 C83901에 감염된 IPEC-J2 세포에서 IL-17C 분비를 거의 완전하게 억제하였습니다. |
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 |
| Solubility | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- 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.)