852230-33-2 Usage
Biological Activity
ml-031 is an agonist of s1p2 with ec50 value of 1 μm [1].sphingosine 1-phosphate (s1p) is a bioactive lysophospholipid mediator mainly released from activated platelets and implicated in many biological responses, such as cell proliferation, migration, survival, and differentiation [1]. sphingolipids belong to a family of bioactive molecules with cell signaling properties. sphingosine 1-phosphate (s1p) is widely expressed on various tissues and cell types. s1p is a pleiotropic lysophospholipid mediator exists in plasma and is released in large amounts from activated platelets [1]. until now, five sphingosine-1-phosphate receptors (s1pr1-s1pr5) have been identified. s1pr4 and s1pr5 are prominently expressed in the immune and nervous systems, respectively. s1p functions by binding to five distinct g protein-coupled receptors, s1p1/edg-1, s1p2/edg-5, s1p3/edg-3, s1p4/edg-6, and s1p5/edg-8.ml-031 activated s1p2 with an ec50 value of 1 μm in a s1p reporter assay [1].
references
[1] satsu h, schaeffer m t, guerrero m, et al. a sphingosine 1-phosphate receptor 2 selective allosteric agonist[j]. bioorganic & medicinal chemistry, 2013, 21(17): 5373-5382.
Check Digit Verification of cas no
The CAS Registry Mumber 852230-33-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,5,2,2,3 and 0 respectively; the second part has 2 digits, 3 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 852230-33:
(8*8)+(7*5)+(6*2)+(5*2)+(4*3)+(3*0)+(2*3)+(1*3)=142
142 % 10 = 2
So 852230-33-2 is a valid CAS Registry Number.
852230-33-2Relevant articles and documents
A sphingosine 1-phosphate receptor 2 selective allosteric agonist
Satsu, Hideo,Schaeffer, Marie-Therese,Guerrero, Miguel,Saldana, Adrian,Eberhart, Christina,Hodder, Peter,Cayanan, Charmagne,Schürer, Stephan,Bhhatarai, Barun,Roberts, Ed,Rosen, Hugh,Brown, Steven J.
, p. 5373 - 5382 (2013/09/02)
Molecular probe tool compounds for the Sphingosine 1-phosphate receptor 2 (S1PR2) are important for investigating the multiple biological processes in which the S1PR2 receptor has been implicated. Amongst these are NF-κB-mediated tumor cell survival and fibroblast chemotaxis to fibronectin. Here we report our efforts to identify selective chemical probes for S1PR2 and their characterization. We employed high throughput screening to identify two compounds which activate the S1PR2 receptor. SAR optimization led to compounds with high nanomolar potency. These compounds, XAX-162 and CYM-5520, are highly selective and do not activate other S1P receptors. Binding of CYM-5520 is not competitive with the antagonist JTE-013. Mutation of receptor residues responsible for binding to the zwitterionic headgroup of sphingosine 1-phosphate (S1P) abolishes S1P activation of the receptor, but not activation by CYM-5520. Competitive binding experiments with radiolabeled S1P demonstrate that CYM-5520 is an allosteric agonist and does not displace the native ligand. Computational modeling suggests that CYM-5520 binds lower in the orthosteric binding pocket, and that co-binding with S1P is energetically well tolerated. In summary, we have identified an allosteric S1PR2 selective agonist compound.
