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L-161982

  Cat. No.:  DC28241   Featured
Chemical Structure
147776-06-5
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More than 5000 active chemicals with high quality for research!
Field of application
L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 147776-06-5
Chemical Name: 2-Thiophenecarboxamide,N-[[4'-[[3-butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]-2-yl]sulfonyl]-3-methyl-
Synonyms: 2-Thiophenecarboxamide,N-[[4'-[[3-butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]-2-yl]sulfonyl]-3-methyl-;2-Thiophenecarboxamide,N-[[4'-[[3-butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-bi;2-Thiophenecarboxamide,N-[[4'-[[3-butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2...;L-161,982;N-[2-[4-[[3-butyl-5-oxo-1-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]phenyl]phenyl]sulfonyl-3-methylthiophene-2-carboxamide;HMS3269M17;N-[[4'-[[3-Butyl-1,5-dihydro-5-oxo-1-[2-(trifluoroMethyl)phenyl]-4H-1,2,4-triazol-4-yl]Methyl][1,1'-biphenyl]-2-yl]sulfonyl]-3-Methyl-2-thiophenecarboxaMide;Peroxy Orange 1;N-[[4'-[[3-Butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]- 2-yl]sulfonyl]-3-methyl-2-thiophenecarboxamide;N-[[4′-[[3-Butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1"-biphenyl]-2-yl]sulfonyl]-3-methyl-2-thiophenecarboxamide
SMILES: C(C1N(CC2C=CC(C3C=CC=CC=3S(NC(C3=C(C)C=CS3)=O)(=O)=O)=CC=2)C(=O)N(C2C=CC=CC=2C(F)(F)F)N=1)CCC
Formula: C32H29F3N4O4S2
M.Wt: 654.722275495529
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice[1][2].
Target: EP4
In Vivo: L-161982 (5 mg/kg; i.p.; once per day for 2 weeks) reduces arthritis lesions and lesion progression in CIA mice[2]. Animal Model: Female DBA/1 mice of 6 to 8 weeks old (collagen-induced arthritis (CIA) mice model)[1] Dosage: 5 mg/kg Administration: i.p.; once per day for 2 weeks Result: Showed less joint swelling and lower arthritis score after 35 days post immunization.
In Vitro: L-161982 (10 μM; 2 hours) blocks PGE2-stimulated cell proliferation of HCA-7 cells[1]. L-161982 (10 μM; 1 hour) blocks PGE2-stimulated ERK phosphorylation in HCA-7 cells[1]. L-161982 induces apoptosis, cell cycle arrest, and inhibits prostaglandin E2-induced proliferation in oral squamous carcinoma Tca8113 cells[3]. Cell Proliferation Assay[1] Cell Line: HCA-7 cells Concentration: 10 μM Incubation Time: 2 hours Result: Blocked PGE2-induced cell proliferation.
References: [1]. Li X, et al.The EP4 antagonist, L-161,982, induces apoptosis, cell cycle arrest, and inhibits prostaglandin E2-induced proliferation in oral squamous carcinoma Tca8113 cells.J Oral Pathol Med. 2017 Nov;46(10):991-997. [2]. Cherukuri DP, et al. The EP4 receptor antagonist, L-161,982, blocks prostaglandin E2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells.Exp Cell Res. 2007 Aug 15;313(14):2969-79. [3]. Chen L, et al. L161982 alleviates collagen-induced arthritis in mice by increasing Treg cells and down-regulating Interleukin-17 and monocyte-chemoattractant protein-1 levels.BMC Musculoskelet Disord. 2017 Nov 16;18(1):462.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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