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SEW-2871 | SEW-2871 : Full agonist of S1PR1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
S1PR1
  • EC50:13 ± 8.58 nm
  • EC50:dose dependent increase (600 nM to 600µM)
  • Activity:13.8x, 5.8x
Full agonist
500 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: SEW2871 was inactive at 10,000 nM on hS1P2, hS1P3, hS1P4, and hS1P ...

Potency
Cellular
In Vitro

S1PR1

Mode of Action: Full agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1074/jbc.M311743200

In Vivo Validations

Mouse
Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 7.1 h
Systemic clearance: 30.7 ml/kg/h
Cmax: 2.0 ug/ml
Tmax: 6 h
Volume of Distribution at Steady-State: 313 ml/kg
Target engagement assay: SEW2871 produced a rapid and dose-dependent peripheral blood lymphopenia after 5 h (ED50 = 5.5 ± 1.04 mg/kg) when tested at doses up to 150 mg/kg.

DOI Reference: 10.1074/jbc.M311743200

Chemical Information

Molecular Formula C20H10F6N2OS
SMILEs FC(F)(F)c1cccc(-c2noc(-c3cc(-c4ccccc4)c(C(F)(F)F)s3)n2)c1
InChI InChI=1S/C20H10F6N2OS/c21-19(22,23)13-8-4-7-12(9-13)17-27-18(29-28-17)15-10-14(11-5-2-1-3-6-11)16(30-15)20(24,25)26/h1-10H
Molecular weight 440.04 Da
AlogP 7.169700000000004
HBond acceptors 3
HBond donors --
Atoms 40

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 21 Nov 2022 )
Cellular Use Rating
In Model Organisms
Historically, SEW2871 was a useful chemical probe as it enabled determination of what S1P receptor isoform drives disruption of lymphocyte trafficking (S1P1) vs. the receptor isoform driving bradycardia...
by SERP
(on 5 Dec 2022 )
Cellular Use Rating
In Model Organisms
SEW-2871 is a potent agonist for S1PR1. Despite showing reasonable selectivity against other S1PR1 subtypes, no further selectivity or off-target data is known (e.g. affinity-based protein profiling target...
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