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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
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Inaccessible (Haz class 6.1), International USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 256414-75-2 Chemical Structure| 256414-75-2

Structure of SEW2871
CAS No.: 256414-75-2

Chemical Structure| 256414-75-2

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SEW2871 is a potent and selective sphingosine-1-phosphate 1 (S1P1) receptor agonist. Activates S1P1 receptor with an EC50 of 13 nM, but does not activate S1P2, S1P3, S1P4 or S1P5 receptors at concentrations up to 10 μM. Cell-permeable and active in vivo.

4.5 *For Research Use Only !

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Product Details of SEW2871

CAS No. :256414-75-2
Formula : C20H10F6N2OS
M.W : 440.36
SMILES Code : FC(C1=CC(C2=NOC(C3=CC(C4=CC=CC=C4)=C(C(F)(F)F)S3)=N2)=CC=C1)(F)F
MDL No. :MFCD00096600
InChI Key :OYMNPJXKQVTQTR-UHFFFAOYSA-N
Pubchem ID :4077460

Safety of SEW2871

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H300
Precautionary Statements:P264-P301+P310
Class:6.1
UN#:2811
Packing Group:

Related Pathways of SEW2871

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human mature oligodendrocytes 100 nM 2 days Induced membrane elaboration Am J Pathol. 2008 Oct;173(4):1143-52
Human ILC3 1 µM 2-3 days Inhibited production of GM-CSF, IL-22, and IL-17 Front Immunol. 2019 Feb 13;10:217
Rat sensory neurons 100 nM 10 min To evaluate the effect of SEW2871 on the excitability of rat sensory neurons, results showed that SEW2871 significantly increased the firing frequency of action potentials. J Neuroinflammation. 2015 Apr 12;12:70
CeL-Sst neurons (Type B) 100 nM 10 minutes SEW2871 significantly depolarized the resting membrane potential and increased input resistance of Type B neurons, but did not change firing frequency. Neuropharmacology. 2022 Feb 1;203:108885
CeL-Sst neurons (Type A) 100 nM 10 minutes SEW2871 did not significantly alter the resting membrane potential or firing frequency of Type A neurons. Neuropharmacology. 2022 Feb 1;203:108885
Immortalized mouse podocytes 1 µM 14 days SEW2871 significantly reduced TNF-α and VEGF mRNA expression in podocytes under high glucose conditions. Kidney Int. 2011 May;79(10):1090-8
Mouse peritoneal macrophages 1 µM 30 minutes SEW2871 stimulates the interaction between SR-B1 and S1PR1-eGFP, similar to HDL, and this interaction was blocked by an inhibitor of SR-B1’s lipid transport activity or an SR-B1 blocking antibody. J Lipid Res. 2024 May;65(5):100541
HEK293A-S1P1-GFP cells 5 µM 30 minutes To evaluate the effect of SEW2871 on S1PR1 internalization. Results showed SEW2871 significantly promoted S1PR1 internalization, which could be blocked by S1PR1 antagonist W146. Cancer Lett. 2021 May 28;506:107-119
Human umbilical vein endothelial cells (HUVEC) 5 µM 30 minutes To evaluate the inhibitory effect of SEW2871 on inflammatory mediator-induced endothelial gap formation. Results showed SEW2871 effectively inhibited BK, VEGF and IL-8 induced endothelial gap formation. Cancer Lett. 2021 May 28;506:107-119
C57BL/6J peritoneal macrophages 1 µM 4 hours SEW2871 significantly reduced LPS-mediated iNOS activity and TNF α secretion and increased Arg I activity, suggesting that the antiinflammatory effects of S1P in macrophages are mediated by the S1P1 receptor. Circ Res. 2008 Apr 25;102(8):950-8

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Streptozotocin-induced diabetic nephropathy model Intraperitoneal injection 0.1 mg/kg Monday to Friday, for 9 weeks SEW2871 significantly reduced urinary albumin excretion and TNF-α levels in diabetic rats, and improved tubular injury and podocyte-specific protein expression. Kidney Int. 2011 May;79(10):1090-8
Rats Thermal hyperalgesia model Intraplantar injection 0.3 μg Single injection, sustained for 5 hours SEW2871 induces thermal hyperalgesia via activation of S1P1 receptor, which can be blocked by the S1P1 receptor antagonist W146 Pain. 2011 Mar;152(3):643-648
Spontaneously hypertensive stroke-prone rats (SHRSP) Unilateral carotid artery occlusion (UCAO) and Japanese permissive diet (JPD) model Intraperitoneal injection 0.5 mg/kg Every other day for 4 weeks SEW2871 significantly reduced lesions in both white and grey matter and ameliorated cerebral blood flow. SEW2871 reversed the loss of endothelial S1PR 1 and tight junction proteins, and significantly attenuated UCAO/JPD induced accumulation of neuronal phosphorylated tau. Aging Dis. 2024 May 21;16(2):1099-1119
Rats Benign prostatic hyperplasia model Intraprostatic injection 0.5 nmol Single injection, duration of 4 weeks SEW2871 led to prostate enlargement in rats iScience. 2024 Oct 30;27(12):111290
Mice ApoM-deficient mice Intraperitoneal injection 10 mg/g Single injection, 150 min prior to imaging SEW2871 rapidly normalized paracellular BBB permeability in Apom-/- mice, and inhibited transcytosis in penetrating arterioles, but not in pial arterioles. Elife. 2019 Nov 25;8:e49405
C57BL/6J mice Epilepsy model Intraperitoneal injection 10 mg/kg Once a day for 48 hours SEW2871 decreased the level of tight junction protein in the hippocampus of epileptic mice, increased blood-brain barrier leakage, and aggravated the severity of seizures compared with the control. Neural Regen Res. 2023 Aug;18(8):1763-1769
Mice Partial hepatectomy (PH) model and bile duct ligation (BDL) model Oral gavage 10 mg/kg/day Once daily for 7 days SEW2871 promotes liver regeneration and alleviates fibrosis by activating endothelial S1P1 signaling. In Apom-/- mice, SEW2871 enhanced the restoration of liver weight, prolonged animal survival, and improved hepatic function recovery. Additionally, SEW2871 reduced fibrosis and thrombosis. Cancer Med. 2020 Oct;9(19):7125-7136
Mice Partial hepatectomy (PH) model and bile duct ligation (BDL) model Oral gavage 10 mg/kg/day Once daily for 7 days SEW2871 promotes liver regeneration and alleviates fibrosis by activating endothelial S1P1 signaling. In Apom-/- mice, SEW2871 enhanced the restoration of liver weight, prolonged animal survival, and improved hepatic function recovery. Additionally, SEW2871 reduced fibrosis and thrombosis. JCI Insight. 2016 Dec 22;1(21):e87058
C57BL/6J male mice Chronic migraine model Intraperitoneal injection 20 mg/kg Once daily for 9 days SEW2871 did not attenuate thermal and mechanical allodynia caused by repeated NTG administration J Headache Pain. 2022 Feb 10;23(1):25
C57BL/6 mice VEGFR blockade-induced emphysema model Gavage 20 mg/kg Once daily for 5 days To evaluate the protective effect of SEW2871 on VEGFR blockade-induced airspace enlargement. Results showed that SEW2871 significantly inhibited airspace enlargement and reduced lung apoptosis. Am J Respir Crit Care Med. 2010 Feb 15;181(4):344-52
Mice Repeated hapten application-induced cutaneous response model Gavage 20 mg/kg Single administration SEW2871 decreased the number of skin-infiltrating eosinophils and reduced the late-phase reaction. Am J Pathol. 2010 Oct;177(4):1881-7
Mice Transverse Aortic Constriction (TAC) model Intraperitoneal injection 3 mg/kg 1 hour before surgery and every 12 hours thereafter for 72 hours To evaluate the protective effects of SEW2871 on cardiac inflammation and function, results showed SEW2871 significantly reduced myocardial inflammation and preserved cardiac function. JCI Insight. 2016 Apr 21;1(5):e85484
Mice CX3CR1-EGFP knock-in mice and CSF1R-EGFP transgenic mice Intravenous injection 5 mg/kg Single dose To evaluate the effect of SEW2871 on monocyte migration in bone tissues, showing that SEW2871 significantly increased the motility of CX3CR1-EGFP positive cells. Nature. 2009 Mar 26;458(7237):524-8
Athymic Foxn1nu nude mice Melanoma lung metastasis model Intraperitoneal injection 5 mg/kg Single dose, 6, 12 or 18 hours before To evaluate the inhibitory effect of SEW2871 on melanoma lung metastasis. Results showed SEW2871 treatment reduced lung metastatic nodules by 65-80%. Cancer Lett. 2021 May 28;506:107-119
Rats Transient middle cerebral artery occlusion model Intraperitoneal injection 5mg/kg Single dose immediately after reperfusion To evaluate the neuroprotective effect of SEW2871 on cerebral ischemia, results showed that SEW2871 significantly reduced infarct volume and improved neurological score Stroke. 2010 Feb;41(2):368-74

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.14mL

22.71mL

4.54mL

2.27mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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