ChemicalBook > CAS DataBase List > L-161,982

L-161,982

Product Name
L-161,982
CAS No.
147776-06-5
Chemical Name
L-161,982
Synonyms
L-161,982;L-161,982 >=98% (HPLC);L-161982, 10 mM in DMSO;L-161,982, EP4 receptor antagonist;colon,cancer,phosphorylation,prostaglandin,Prostaglandin Receptor,L161982,arthritis,inhibit,proliferation,L 161982,L-161982,Inhibitor;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;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;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-
CBNumber
CB31074878
Molecular Formula
C32H29F3N4O4S2
Formula Weight
654.72
MOL File
147776-06-5.mol
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L-161,982 Property

Density 
1.37±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: soluble15mg/mL, clear
form 
powder
pka
4.57±0.10(Predicted)
color 
white to beige
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0690
Product name
L-161,982
Purity
≥98% (HPLC)
Packaging
5mg
Price
$162.45
Updated
2025/07/31
Sigma-Aldrich
Product number
SML0690
Product name
L-161,982
Purity
≥98% (HPLC)
Packaging
25mg
Price
$683
Updated
2025/07/31
Cayman Chemical
Product number
10011565
Product name
L-161,982
Purity
≥95%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
10011565
Product name
L-161,982
Purity
≥95%
Packaging
5mg
Price
$161
Updated
2024/03/01
Cayman Chemical
Product number
10011565
Product name
L-161,982
Purity
≥95%
Packaging
25mg
Price
$704
Updated
2024/03/01
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L-161,982 Chemical Properties,Usage,Production

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.

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.

Definition

ChEBI: 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 is a member of biphenyls.

Biological Activity

EP 4 receptor antagonist that is selective over all other members of the prostanoid receptor family (K i values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μ M for human EP 4 , TP, EP 3 , DP, FP, IP, EP 1 and EP 2 receptors respectively). Suppresses PGE 2 -induced bone formation in rats and prevents the nociceptive response induced by misoprostol in formalin-injected mice.

Biochem/physiol Actions

L-161,982 is a potent EP4 receptor antagonist that is selective over all other members of the prostanoid receptor family (Ki values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μM for human EP4, TP, EP3, DP, FP, IP, EP1 and EP2 receptors respectively.

storage

Desiccate at +4°C

References

[1] M. MACHWATE. Prostaglandin receptor EP(4) mediates the bone anabolic effects of PGE(2).[J]. Molecular Pharmacology, 2001, 60 1 1: 36-41. DOI: 10.1124/mol.60.1.36
[2] KIYOSHI TAKAYAMA. Prostaglandin E2 suppresses chemokine production in human macrophages through the EP4 receptor.[J]. The Journal of Biological Chemistry, 2002, 277 46: 44147-44154. DOI: 10.1074/jbc.m204810200
[3] DURGA PRASAD CHERUKURI . The EP4 receptor antagonist, L-161,982, blocks prostaglandin E2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells[J]. Experimental cell research, 2007, 313 14: Pages 2969-2979. DOI: 10.1016/j.yexcr.2007.06.004
[4] ANG LIN. TLR4 signaling promotes a COX-2/PGE2/STAT3 positive feedback loop in hepatocellular carcinoma (HCC) cells[J]. Oncoimmunology, 2015, 5 1. DOI: 10.1080/2162402x.2015.1074376

L-161,982 Preparation Products And Raw materials

Raw materials

Preparation Products

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L-161,982 Suppliers

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147776-06-5, L-161,982Related Search:

CJ-21058 GW 627368X CJ-42794 Grapiprant PROSTAGLANDIN F1ALPHA Latanoprost Misoprostol Acid ONO-AE3-208 13,14-DIHYDROPROSTAGLANDIN E1 Prostaglandin F2a PROSTAGLANDIN D2 6(R)-(4-CARBOXYPHENYLTHIO)-5(S)-HYDROXY-7(E),9(E),11(Z),14(Z)-EICOSATETRAENOIC ACID 11BETA-PROSTAGL AND IN F2ALPHA LEUKOTRIENE B4 DIMETHYL AMIDE LEUKOTRIENE D4 CJ 033466 L-161,982 4,5-DIETHYL-2,4-DIHYDRO 1,2,4-TRIAZOL-3 ONE

  • L-161,982
  • 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-[2-[4-[[3-butyl-5-oxo-1-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]phenyl]phenyl]sulfonyl-3-methylthiophene-2-carboxamide
  • 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-
  • L-161,982 >=98% (HPLC)
  • colon,cancer,phosphorylation,prostaglandin,Prostaglandin Receptor,L161982,arthritis,inhibit,proliferation,L 161982,L-161982,Inhibitor
  • L-161,982, EP4 receptor antagonist
  • L-161982, 10 mM in DMSO
  • 147776-06-5
  • C32H29F3N4O4S2
  • Prostanoid receptor and related