APD334 - CAS 1206123-37-6
Catalog number: 1206123-37-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Sphingosine 1 Phosphate Receptor
This active moleclar is a Sphingosine 1 Phosphate Receptor antagonists for treatment of multiple sclerosis (MS) and other autoimmune diseases originated by Arena Pharmaceuticals. APD334 was efficacious in a mouse EAE (experimental autoimmune encephalomyelitis ) model of MS and a rat CIA (collagen induced arthritis) model. It was found to have appreciable central exposure. In Sep 2015, Arena Pharmaceuticals planed a phase II extension trial for Ulcerative colitis in USA was on-going. In Mar 2016, Arena Pharmaceuticals had patent protection for APD 334 in USA, Japan, China, Australia and Russia.
APD334; APD 334; APD-334; Etrasimod; UNII-6WH8495MMH; 6WH8495MMH; CHEMBL3358920;2-[(3R)-7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
Soluble in DMSO
-20°C Freezer
multiple sclerosis (MS) and other autoimmune diseases.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Originator: Arena Pharmaceuticals
1.Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Buzard DJ;Kim SH;Lopez L;Kawasaki A;Zhu X;Moody J;Thoresen L;Calderon I;Ullman B;Han S;Lehmann J;Gharbaoui T;Sengupta D;Calvano L;Montalban AG;Ma YA;Sage C;Gao Y;Semple G;Edwards J;Barden J;Morgan M;Chen W;Usmani K;Chen C;Sadeque A;Christopher RJ;Thatte J;Fu L;Solomon M;Mills D;Whelan K;Al-Shamma H;Gatlin J;Le M;Gaidarov I;Anthony T;Unett DJ;Blackburn A;Rueter J;Stirn S;Behan DP;Jones RM ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7. doi: 10.1021/ml500389m. eCollection 2014 Dec 11.
APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases. APD334 is a potent functional antagonist of S1P1 and has a favorable PK/PD profile, producing robust lymphocyte lowering at relatively low plasma concentrations in several preclinical species. This new agent was efficacious in a mouse experimental autoimmune encephalomyelitis (EAE) model of MS and a rat collagen induced arthritis (CIA) model and was found to have appreciable central exposure.
2.Will novel oral formulations change the management of inflammatory bowel disease?
Nielsen OH;Seidelin JB;Ainsworth M;Coskun M Expert Opin Investig Drugs. 2016 Jun;25(6):709-18. doi: 10.1517/13543784.2016.1165204. Epub 2016 Mar 28.
INTRODUCTION: ;The traditional management of inflammatory bowel disease (IBD) with sulphasalazine/5-aminosalicylic acid, glucocorticoids and immunomodulators (i.e., thiopurines and methotrexate) was nearly two decades ago extended with intravenously or subcutaneously administered biologics (i.e., tumor necrosis factor inhibitors and later gut-selective integrin antagonists). However, recently, orally administered treatments with simple, well-characterized, and stable structures consisting of either small molecules or anti-sense therapy have been devised.;AREAS COVERED: ;This review discusses the current approaches with promising new oral drugs with distinct modes of action, including: the Janus kinase inhibitors (i.e., tofacitinib, filgotinib and peficitinib); the immunomodulatory drug (laquinimod); a small α4 antagonist (AJM300); agonists for sphingosine-phosphate receptors (i.e., ozanimod, APD334, and amiselimod), as well as anti-sense therapy (mongersen) targeting SMAD7, drugs which directly target intracellular pathways of relevance for intestinal inflammation.;EXPERT OPINION: ;A new avenue using easily administered oral therapies for the management of IBD is being introduced. While their place in the clinical armamentarium remains to be proven, it is likely that many of these drugs will find their place in the treatment algorithm of IBD in the next few years.
3.Modulation of sphingosine-1-phosphate in inflammatory bowel disease.
Peyrin-Biroulet L;Christopher R;Behan D;Lassen C Autoimmun Rev. 2017 May;16(5):495-503. doi: 10.1016/j.autrev.2017.03.007. Epub 2017 Mar 7.
Inflammatory bowel diseases (IBD), including ulcerative colitis and Crohn's disease, involve an inappropriate immune reaction in the digestive tract, causing a variety of disabling symptoms. The advent of monoclonal antibodies (anti-tumor necrosis factor, anti-integrin, anti-interleukin -23) has revolutionized IBD management. Nevertheless, these agents, with potential for immunogenicity, are associated with high rates of response loss and disease relapse over time. They are also associated with high production costs. Sphingosine-1-phosphate (S1P), a membrane-derived lysophospholipid signaling molecule, is implicated in a vast array of physiological and pathophysiological processes, primarily via extracellular activation of S1P1-S1P5 receptors. S1P1, S1P4 and S1P5 are involved in regulation of the immune system, while S1P2 and S1P3 may be associated with cardiovascular, pulmonary, and theoretical cancer-related risks. Targeting S1P receptors for inflammatory conditions has been successful in clinical trials leading to approval of the non-selective S1P modulator, fingolimod, for relapsing forms of multiple sclerosis. However, the association of this non-selective S1P modulator with serious adverse events provides the rationale for developing more selective S1P receptor modulators.
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