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Chemical Structure| 1841460-82-9 Chemical Structure| 1841460-82-9

Structure of TH1020
CAS No.: 1841460-82-9

Chemical Structure| 1841460-82-9

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TH1020 is Toll-like receptor (TLR) 5/Flagellin complex antagonist with IC50 of 0.85 μM. TH1020 competes with flagellin for TLR5 binding to inhibit the TLR5:flagellin interaction and subsequent downstream TNF-α secretion.

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Product Citations

Product Citations

Tang, Lingwei ; Pan, Deng ; Wang, Yizhen ; Yao, Shuxia ; Qian, Xueru ; Huang, Chigang , et al.

Abstract: Eutrophication significantly impacts on aquatic ecosystems. The accumulation of nutrients such as nitrogen and phosphorus in water bodies leads to a series of ecological problems, including water quality deterioration, reduced dissolved oxygen levels, and decreased transparency. These issues significantly impact the physical and chemical properties of water bodies, the diversity of aquatic organisms, community structure, and ecological functions. Carassius cuvieri (CC) and Triploid Crucian carp No. 2 (TCC) are common freshwater aquaculture fish species with extensive farming foundations and economic value. Their survival and growth are closely tied to environment conditions. This study uses CC and Triploid TCC as research subjects, conducting a 30-day eutrophication aquaculture experiment in a mildly eutrophic water body (TN: 0.868 mg/L; TP: 0 mg/L) as the initial environment. Combining morphological, histological, transcriptomic, inhibitor-treatment, and qRT-PCR techniques, we explored the molecular mechanisms underlying the adaptation of crucian carp to eutrophication environments. The results showed that, as the degree of eutrophication increased, growth indices of both CC and TCC were affected to varying degrees. Peripheral blood cell and histological section observations revealed abnormal blood cell morphology, increased white blood cell counts, nuclear displacement and aggregation in hepatocytes, curved and thinned gill filaments, and broken and damaged gill filaments in both fish species; High-throughput sequencing results showed that differentially expressed genes in liver tissue were primarily enriched in immune-mediated infectious-diseases, lipid-metabolism, and signal -transduction pathways. mRNA expression analysis of crucian carp embryos treated with the TLR5 inhibitor suggested that changes in certain genes within the TLRs signaling pathway may be associated with the activation of downstream cascades and the secretion of pro-inflammatory cytokines, collectively facilitating fish adaptation eutrophication. This study provides scientific experimental evidence for optimising large-scale fish farming models, monitoring of aquaculture environmental quality, and maintaining the balance of aquatic ecosystems. TCC copes better with eutrophication through stronger and immune responses, whereas CC shows more pronounced gill and liver damage.

Keywords: Eutrophication ; Crucian carp ; Transcriptomics ; Adaptation mechanisms

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Product Details of TH1020

CAS No. :1841460-82-9
Formula : C23H15N7S2
M.W : 453.54
SMILES Code : C12=NC=NC(SC3=NN=C(C4=CC=NC=C4)N3CC5=CC=CC=C5)=C1SC6=NC=CC=C62
MDL No. :MFCD30480930
InChI Key :CBBXTGWSGPEJEE-UHFFFAOYSA-N
Pubchem ID :124203921

Safety of TH1020

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319
Precautionary Statements:P264-P280-P302+P352-P305+P351+P338-P332+P313-P337+P313-P362

Related Pathways of TH1020

pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human dermal fibroblasts (HDFs) 1.5, 3, 6 µM 1-hour pretreatment To evaluate the inhibitory effect of TH1020 on FLA-AA-induced cytokine secretion, a dose-dependent reduction in IL-8 and IL-6 secretion was observed Int J Mol Sci. 2021 Jun 28;22(13):6920
THP-1 macrophages 1.5, 3, 6 µM 1-hour pretreatment To evaluate the inhibitory effect of TH1020 on FLA-AA-induced cytokine secretion, a dose-dependent reduction in IL-8 and TNF-α secretion was observed Int J Mol Sci. 2021 Jun 28;22(13):6920

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.02mL

2.20mL

1.10mL

22.05mL

4.41mL

2.20mL

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