Chemical Property of N-[2-[4-[[3-butyl-5-oxo-1-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]phenyl]phenyl]sulfonyl-3-methyl-2-thiophenecarboxamide
Chemical Property:
- Refractive Index:1.633
- Boiling Point:°Cat760mmHg
- Flash Point:°C
- PSA:139.68000
- Density:1.37g/cm3
- LogP:8.07100
- Storage Temp.:Desiccate at +4°C
- Solubility.:DMSO: soluble15mg/mL, clear
- XLogP3:7.3
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:9
- Rotatable Bond Count:10
- Exact Mass:654.15823225
- Heavy Atom Count:45
- Complexity:1190
- Purity/Quality:
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98%,99%, *data from raw suppliers
L-161,982 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CCCCC1=NN(C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3S(=O)(=O)NC(=O)C4=C(C=CS4)C)C5=CC=CC=C5C(F)(F)F
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Description
Prostaglandin E2 (PGE2) exerts its effects through four separate G coupled-protein receptors (EP1-4). L-161,982 is a potent and selective EP4 receptor antagonist. It demonstrates selective binding to human EP4 receptors with a Ki value of 0.024 μM compared to other receptors of the prostanoid family, EP1, EP2, EP3, DP, FP, and IP, with Ki values of 17, 23, 1.9, 5.1, 5.6, and 6.7 μM, respectively. L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages. At 10 μM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells.
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Uses
L-161,982 is an EP4 receptor antagonist, which blocks prostaglandin E2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells.