147776-06-5 Usage
Description
L-161,982 is a potent and selective EP4 receptor antagonist, which blocks prostaglandin E2 (PGE2)-induced signal transduction and cell proliferation. It demonstrates selective binding to human EP4 receptors with a Ki value of 0.024 μM, compared to other receptors of the prostanoid family, such as EP1, EP2, EP3, DP, FP, and IP, with Ki values ranging from 1.9 to 23 μM. L-161,982 has been shown to suppress PGE2-stimulated bone formation in young rats and reverse the anti-inflammatory action of PGE2 in LPS-activated human macrophages.
Uses
Used in Pharmaceutical Industry:
L-161,982 is used as an EP4 receptor antagonist for blocking PGE2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells. This application is particularly relevant in the development of targeted therapies for colon cancer and potentially other cancer types where PGE2 plays a role in promoting cell growth and survival.
Additionally, L-161,982 can be used as a research tool to study the role of EP4 receptors in various biological processes, such as inflammation, bone formation, and cancer progression. This can help in the development of new therapeutic strategies and a better understanding of the underlying mechanisms involved in these conditions.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 147776-06-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,4,7,7,7 and 6 respectively; the second part has 2 digits, 0 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 147776-06:
(8*1)+(7*4)+(6*7)+(5*7)+(4*7)+(3*6)+(2*0)+(1*6)=165
165 % 10 = 5
So 147776-06-5 is a valid CAS Registry Number.
InChI:InChI=1/C32H29F3N4O4S2/c1-3-4-13-28-36-39(26-11-7-6-10-25(26)32(33,34)35)31(41)38(28)20-22-14-16-23(17-15-22)24-9-5-8-12-27(24)45(42,43)37-30(40)29-21(2)18-19-44-29/h5-12,14-19H,3-4,13,20H2,1-2H3,(H,37,40)
147776-06-5Relevant articles and documents
Triazolinone Biphenylsulfonamide Derivatives as Orally Active Angiotensin II Antagonists with Potent AT1 Receptor Affinity and Enhanced AT2 Affinity
Ashton, Wallace T.,Chang, Linda L.,Flanagan, Kelly L.,Hutchins, Steven M.,Naylor, Elizabeth M.,et al.
, p. 2808 - 2826 (2007/10/02)
Several series of 2,4-dihydro-2,4,5-trisubstituted-3H-1,2,4-triazol-3-ones with acidic sulfonamide replacements of tetrazole at the 2'-position of the biphenyl-4-ylmethyl side chain at N4 were prepared and tested as angiotensin II (AII) antagon
