355025-24-0 Usage
Description
Lysophosphatidic acid (LPA) is a bioactive lipid mediator that signals through five distinct G protein-coupled receptors (LPA1-5). Ki16425 is a LPA receptor antagonist with selectivity for LPA1 and LPA3. It exhibits Ki values of 0.34, 6.5, and 0.93 μM for the human LPA1, LPA2, and LPA3 receptors, respectively, as determined by measuring inositol phosphate production in RH7777-transfected cells. Ki1642, at 10 μM, significantly blocks the response of a variety of cancer cell lines to LPA-induced cell migration.
Uses
Different sources of media describe the Uses of 355025-24-0 differently. You can refer to the following data:
1. Ki 16425 has been used as a chemical inhibitor to study the regulation of LPA (lysophosphatidic acid) on LPAR(LPA receptor) subtypes.
2. Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3.
Biochem/physiol Actions
Ki 16425 possesses a short-lived inhibitory activity. It has been studied that Ki 16425 is effective in the inhibition of neuropathic pain‐like behaviors.
references
[1]. ohta h, sato k, murata n, damirin a, malchinkhuu e, kon j, kimura t, tobo m, yamazaki y, watanabe t, yagi m, sato m, suzuki r, murooka h, sakai t, nishitoba t, im ds, nochi h, tamoto k, tomura h, okajima f. ki16425, a subtype-selective antagonist for edg-family lysophosphatidic acid receptors. mol pharmacol. 2003 oct;64(4):994-1005.[2]. ruisanchez é, dancs p, kerék m, németh t, faragó b, balogh a, patil r, jennings bl, liliom k, malik ku, smrcka av, tigyi g, benyó z. lysophosphatidic acid induces vasodilation mediated by lpa1 receptors, phospholipase c, and endothelial nitric oxide synthase. faseb j. 2014 feb;28(2):880-90. [3]. su sc, hu x, kenney pa, merrill mm, babaian kn, zhang xy, maity t, yang sf, lin x, wood cg. autotaxin-lysophosphatidic acid signaling axis mediates tumorigenesis and development of acquired resistance to sunitinib in renal cell carcinoma. clin cancer res. 2013 dec 1;19(23):6461-72. [4]. david m, sahay d, mege f, descotes f, leblanc r, ribeiro j, clézardin p, peyruchaud o. identification of heparin-binding egf-like growth factor (hb-egf) as a biomarker for lysophosphatidic acid receptor type 1 (lpa1) activation in human breast and prostate cancers. plos one. 2014 may 14;9(5):e97771.
Check Digit Verification of cas no
The CAS Registry Mumber 355025-24-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,5,5,0,2 and 5 respectively; the second part has 2 digits, 2 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 355025-24:
(8*3)+(7*5)+(6*5)+(5*0)+(4*2)+(3*5)+(2*2)+(1*4)=120
120 % 10 = 0
So 355025-24-0 is a valid CAS Registry Number.
355025-24-0Relevant articles and documents
Synthesis and biological evaluation of optically active Ki16425
Sato, Takanao,Sugimoto, Kenji,Inoue, Asuka,Okudaira, Shinichi,Aoki, Junken,Tokuyama, Hidetoshi
, p. 4323 - 4326 (2012/09/22)
An enantionselective synthesis of both enantiomers of Ki16425, which possesses selective LPA antagonistic activity, was achieved. The isoxazole core was constructed by a 1,3-dipolar cycloaddition of nitrile oxide with alkyne and condensation with the optically active α-phenethyl alcohol segment, which was prepared by an enantioselective reduction of arylmethylketone. Biological evaluation of both enantiomers of Ki16425 revealed that the (R)-isomer showed much higher antagonistic activity for LPA1 and LPA3 receptors.
