CysLT1 Inhibitors
CysLT1 inhibitors are a class of chemical compounds that specifically target and inhibit the activity of the CysLT1 receptor, a G protein-coupled receptor (GPCR) that is primarily involved in mediating the effects of cysteinyl leukotrienes (CysLTs). Cysteinyl leukotrienes, including LTC4, LTD4, and LTE4, are lipid signaling molecules derived from arachidonic acid through the lipoxygenase pathway. These molecules play significant roles in various physiological processes, particularly in the immune system where they are involved in mediating inflammation and allergic responses. The CysLT1 receptor is one of the key receptors for CysLTs, and it is predominantly expressed on the surface of certain immune cells, such as eosinophils, mast cells, and smooth muscle cells in the airways and vasculature. Activation of the CysLT1 receptor by its ligands leads to a cascade of intracellular signaling events that result in bronchoconstriction, increased vascular permeability, and the recruitment of immune cells to sites of inflammation.
Inhibitors of CysLT1 are typically small molecules designed to bind to the receptor, blocking the interaction between the receptor and its natural ligands, cysteinyl leukotrienes. By preventing this interaction, CysLT1 inhibitors can effectively disrupt the downstream signaling pathways that would normally be triggered by CysLT1 activation. The development of CysLT1 inhibitors involves detailed studies of the receptor's structure, particularly the ligand-binding sites, to identify critical regions where these inhibitors can interact and exert their effects. By inhibiting CysLT1, researchers can explore the receptor's role in mediating various physiological and pathological processes, particularly those related to immune responses and inflammation. The study of CysLT1 inhibitors is important for understanding how this receptor contributes to the broader network of signaling pathways in the body, particularly in contexts where CysLTs play a significant role. This research enhances our understanding of the molecular mechanisms underlying the actions of cysteinyl leukotrienes and the potential for modulating these pathways through targeted inhibition of their receptors.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $36.00 $68.00 $107.00 $214.00 $234.00 $862.00 $1968.00 | 47 | |
Curcumin has been observed to suppress the expression of CysLT1 by inhibiting the activation of the transcription factor NF-κB within the nucleus, which is crucial for the expression of many inflammation-related genes including CysLT1. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $60.00 $185.00 $365.00 | 64 | |
Resveratrol may decrease CysLT1 expression by activating SIRT1, an NAD+-dependent deacetylase that can deacetylate transcription factors involved in inflammatory response pathways, subsequently leading to a reduction in CysLT1 gene transcription. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $108.00 $245.00 $918.00 $49.00 | 33 | |
Quercetin could reduce CysLT1 expression through the inhibition of Janus kinase (JAK) enzymes, which are involved in the activation of STAT proteins that promote the expression of inflammatory genes. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $42.00 $72.00 $124.00 $238.00 $520.00 $1234.00 | 11 | |
Epigallocatechin Gallate may suppress CysLT1 expression by hindering the phosphorylation of the epidermal growth factor receptor (EGFR), which can initiate a signaling cascade that includes the expression of pro-inflammatory genes. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $26.00 $92.00 $120.00 $310.00 $500.00 $908.00 $1821.00 | 46 | |
Genistein has the potential to decrease CysLT1 expression by inhibiting protein tyrosine kinases, thereby reducing the activity of transcription factors that drive the expression of inflammatory mediators. | ||||||
Methotrexate | 59-05-2 | sc-3507 sc-3507A | 100 mg 500 mg | $92.00 $209.00 | 33 | |
Methotrexate may reduce the expression of CysLT1 by inhibiting the enzyme dihydrofolate reductase, leading to decreased availability of folate and subsequent downregulation of nucleotide synthesis which is essential for gene expression. | ||||||
D,L-Sulforaphane | 4478-93-7 | sc-207495A sc-207495B sc-207495C sc-207495 sc-207495E sc-207495D | 5 mg 10 mg 25 mg 1 g 10 g 250 mg | $150.00 $286.00 $479.00 $1299.00 $8299.00 $915.00 | 22 | |
DL-Sulforaphane could inhibit CysLT1 expression by enhancing the transcription of antioxidant response element (ARE)-driven genes, which can suppress the oxidative stress-related activation of inflammatory pathways responsible for CysLT1 expression. | ||||||
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $65.00 $319.00 $575.00 $998.00 | 28 | |
Retinoic acid may downregulate CysLT1 expression through the retinoic acid receptor (RAR)-mediated inhibition of AP-1, a transcription factor involved in the expression of multiple genes during inflammatory processes. | ||||||
1α,25-Dihydroxyvitamin D3 | 32222-06-3 | sc-202877B sc-202877A sc-202877C sc-202877D sc-202877 | 50 µg 1 mg 5 mg 10 mg 100 µg | $325.00 $632.00 $1428.00 $2450.00 $400.00 | 32 | |
Calcitriol, the active form of Vitamin D, may decrease the expression of CysLT1 by binding to the vitamin D receptor (VDR) and hindering the activation of NF-κB, which is a key regulator of inflammatory gene expression. | ||||||
Pioglitazone | 111025-46-8 | sc-202289 sc-202289A | 1 mg 5 mg | $54.00 $123.00 | 13 | |
Pioglitazone may suppress CysLT1 expression through activation of PPARγ, which can lead to the transcriptional upregulation of anti-inflammatory genes that work to shut down inflammatory gene expression cascades, including those related to CysLT1. | ||||||