125248-71-7 Purity
97%
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Specification
The freshly isolated human peripheral mononuclear blood cells (PBMCs) were used for expression analysis by flow cytometry in order to analyze the expression of the human G protein-coupled bitter taste receptor T2R38 in resting and activated lymphocytes and T cell subsets. The functional relevance of the receptor on lymphocytes was investigated using goitrin in a calcium-based assay. After goitrin treatment, TNF-alpha secretion was quantified in PBMCs with functional and non-functional T2R38 receptors.
Goitrin-related experiments and results
· The effects of the natural T2R38 agonist Goitrin on donor human PBMCs with a functional T2R38 PAV haplotype were investigated by flow cytometry.
Calcium flux was measured in lymphocytes treated with Fluo-4 AM (FEm: 516 nm) and showed a concentration-dependent response to goitrin, beginning at concentrations exceeding 20 μM. At a concentration of 100 μM, goitrin induced a 144% increase in calcium flux compared to the solvent control. Pretreating the cells with the specific PLCβ-2 inhibitor U-73122 prior to the addition of 100 μM goitrin effectively blocked the calcium flux.
· Subsequently, the effect of goitrin on the secretion of the strong pro-inflammatory cytokine TNF-alpha was assessed. In PBMCs expressing either the functional (PAV haplotype) or non-functional (AVI/AVI diplotype) T2R38 receptor, it was observed distinct responses to goitrin. While goitrin had no impact on TNF-alpha secretion in samples with the non-functional T2R38 receptor, it significantly inhibited TNF-alpha release in samples from donors with the functional T2R38, in comparison to the solvent control.
The molecular formula of DL-Goitrin is C5H7NOS.
DL-Goitrin was created on 2005-03-27 and modified on 2023-12-30.
The molecular weight of DL-Goitrin is 129.18 g/mol.
The IUPAC name of DL-Goitrin is 5-ethenyl-1,3-oxazolidine-2-thione.
The InChIKey of DL-Goitrin is UZQVYLOFLQICCT-UHFFFAOYSA-N.
DL-Goitrin has one hydrogen bond donor count.
The topological polar surface area of DL-Goitrin is 53.4 2.
DL-Goitrin contains 8 heavy atoms.
The formal charge of DL-Goitrin is 0.
DL-Goitrin has 0 defined atom stereocenter counts.