SEW 2871 - CAS 256414-75-2
Catalog number: 256414-75-2
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
SEW 2871 is a potent, cell-permeable and selective sphingosine-1-phosphate type 1 receptor agonist (EC50= 13 nM). SEW 2871 suppresses the immune response by decreasing the number of lymphocytes circulating in blood without causing bradycardia.
Solid powder
5-[4-Phenyl-5-(trifluoromethyl)thiophen-2-yl]-3-[3-(trifluoromethyl)phenyl]1,2,4-oxadiazole; SEW2871; SEW2871; SEW2871
Soluble to 20 mM in DMSO and to 20 mM in ethanol
Boiling Point:
654.6±55.0 ℃ at 760 mmHg
1.2±0.1 g/cm3
Canonical SMILES:
1.Sphingosine-1-phosphate receptors mediate neuromodulatory functions in the CNS.
Sim-Selley LJ;Goforth PB;Mba MU;Macdonald TL;Lynch KR;Milstien S;Spiegel S;Satin LS;Welch SP;Selley DE J Neurochem. 2009 Aug;110(4):1191-202. doi: 10.1111/j.1471-4159.2009.06202.x. Epub 2009 May 31.
Sphingosine-1-phosphate (S1P) is a ubiquitous, lipophilic cellular mediator that acts in part by activation of G-protein-coupled receptor. Modulation of S1P signaling is an emerging pharmacotherapeutic target for immunomodulatory drugs. Although multiple S1P receptor types exist in the CNS, little is known about their function. Here, we report that S1P stimulated G-protein activity in the CNS, and results from [(35)S]GTPgammaS autoradiography using the S1P(1)-selective agonist SEW2871 and the S1P(1/3)-selective antagonist VPC44116 show that in several regions a majority of this activity is mediated by S1P(1) receptors. S1P receptor activation inhibited glutamatergic neurotransmission as determined by electrophysiological recordings in cortical neurons in vitro, and this effect was mimicked by SEW2871 and inhibited by VPC44116. Moreover, central administration of S1P produced in vivo effects resembling the actions of cannabinoids, including thermal antinociception, hypothermia, catalepsy and hypolocomotion, but these actions were independent of CB(1) receptors. At least one of the central effects of S1P, thermal antinociception, is also at least partly S1P(1) receptor mediated because it was produced by SEW2871 and attenuated by VPC44116.
2.A selective sphingosine-1-phosphate receptor 1 agonist SEW-2871 aggravates gastric cancer by recruiting myeloid-derived suppressor cells.
Zhou Y;Guo F J Biochem. 2018 Jan 1;163(1):77-83. doi: 10.1093/jb/mvx064.
The immune status of tumor microenvironment in gastric cancer is poorly understood, which limits the development of novel strategies in this field. Sphingosine-1-phosphate (S1P) acts as an immune modulator, but the role of S1P in gastric cancer is elusive. Here, we aim to investigate S1P receptor 1 (S1P1)-mediated effect of S1P in gastric cancer. We generated a xenograft mouse model and used SEW-2871, a S1P1 specific agonist to activate S1P1 signalling. Tumor-infiltrating lymphocytes (TILs) were isolated and analysed using flow cytometry. Chemokine expression of tumor cells was evaluated using quantitative real-time polymerase chain reaction. Myeloid-derived suppressor cells (MDSCs) migration was assessed using Transwell chambers. SEW-2871 promoted tumor growth in our mouse model, and induced a higher level of MDSC and a reduced level of CD8+CD69+ T cells within tumor. Consistently, the anti-tumoral function of cytotoxic T lymphocytes was impaired in mice with SEW-2871 treatment. Additionally, SEW-2871 enhanced expression of several MDSC recruitment-associated chemokines (CXCL12, CXCL5 and CCL2) in tumor cells. These chemokines facilitated MDSC migration by interaction with CCR2, CXCR2 and CXCR4.
3.Sphingosine kinases/sphingosine-1-phosphate and death Signalling in APP-transfected cells.
Gassowska M;Cieslik M;Wilkaniec A;Strosznajder JB Neurochem Res. 2014 Apr;39(4):645-52. doi: 10.1007/s11064-014-1240-3. Epub 2014 Jan 23.
It has been postulated that disturbances in the sphingolipid metabolism play a key role in the pathogenesis of Alzheimer's disease (AD). An alteration in sphingosine kinases 1, 2 (SphK1/2) and sphingosine-1-phosphate (S1P) was recently reported in AD. However, the effect of AD-related amyloid beta (Aβ) peptides on SphK1/2 and the role of S1P in Aβ toxicity have not been fully elucidated. In this study the relationship between the Aβ concentration and SphK1/2 expression/activity was analysed in PC12 cells transfected with the Aβ precursor protein, wild-type (APPwt) or bearing a double Swedish mutation (APPsw). The role of SphK(s)/S1P in cell survival and death was also investigated. Our results indicated that endogenously liberated Aβ significantly decreases expression and activity of SphK1/2. The SphK(s) inhibitor (SKI II, 10 μM) decreased the viability of APPwt, APPsw as well as empty vector-transfected PC12 control cells. Our data demonstrated that expression of S1P receptor-1 (S1P1) was significantly reduced in APP-transfected cells. The effect of S1P applied exogenously was cell type-dependent. In control and APPwt cells S1P reduced the effect of the SphK1 inhibitor on death signalling.
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CAS 256414-75-2 SEW 2871

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