147776-06-5

147776-06-5 structure

Name: L-161,982
Chemical Name: 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
CAS Number: 147776-06-5
Molecular Formula: C₃₂H₂₉F₃N₄O₄S₂
Molecular Weight: 654.72200
Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
Create Date: 2016-05-29 13:46:25
Modify Date: 2024-01-02 10:51:00
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].

Name	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
Synonyms	L-161,982 HMS3269M17 Peroxy Orange 1

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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor Research Areas >> Inflammation/Immunology
Target	EP4
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.
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.
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.

Density	1.37g/cm3
Melting Point	> 145 °C
Molecular Formula	C₃₂H₂₉F₃N₄O₄S₂
Molecular Weight	654.72200
Exact Mass	654.15800
PSA	139.68000
LogP	8.07100
Index of Refraction	1.633
Storage condition	2-8°C

RIDADR	NONH for all modes of transport

147776-06-5	54944-41-1
308277-46-5	22834-80-6
105381-36-0	17688-29-8
2072-71-1	100324-91-2
3164-29-2	362049-59-0