Chemical Structure : BTI-A-404
CAS No.:
537679-57-5
BTI-A-404
Catalog No.: PC-24797Not For Human Use, Lab Use Only.
BTI-A-404 is a selective and potent competitive inverse agonist / antagonist of human GPR43 (FFA2R) with cAMP IC50 of 9.5 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BTI-A-404 is a selective and potent competitive inverse agonist / antagonist of human GPR43 (FFA2R) with cAMP IC50 of 9.5 uM.
BTI-A-404 increased intracellular level of cAMP (IC50=9.5 uM) and reversed the effect of propionate on cAMP production only in the presence of hGPR43 in Glosensor cell line, but not in Glosensor cells without hGPR43.
BTI-A-404 is still able to increase cAMP with both of IC50 of 2.1 μM only in the GPR43-overexpressing cells.
BTI-A-404 is inactive against hGPR41 and hChemR23 at concentrations up to 50 μM, also does not inhibits mGPR43.
BTI-A-404 significantly induced the secretion of GLP-1 in NCI-H716 cells.
Physicochemical Properties
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M.Wt
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378.48
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Formula
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C22H26N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-[4-(dimethylamino)phenyl]-N-(3,5-dimethylphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydro-5-pyrimidinecarboxamide
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References
1. Park BO, et al. Eur J Pharmacol. 2016 Jan 15;771:1-9.
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