PF-462991
PF-462991 (PF-991) is a S1P1 receptor agonist with an EC50 of 1.9 nM. PF-462991 functionally activates this receptor via the β-arrestin pathway. PF-462991 is applicable to research related to rheumatoid arthritis.
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- CAS. Nr.: 1149727-90-1
- Formel: C25H29N3O3
- Molecular Weight:419.53
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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S1PR1 1.9 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | EC50 |
>10 μM
Compound: PF-991
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Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
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[PMID: 26687487] |
| U2OS | EC50 |
1.9 nM
Compound: PF-991
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Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
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[PMID: 26687487] |
PF-462991 potently activates the S1P1 receptor with an EC50 of 1.9 nM; in β-arrestin functional assays, its selectivity for the S1P1 receptor is over 5263-fold higher than that for the S1P3 receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1149727-90-1
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Molecular Weight 419.53
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Formel C25H29N3O3
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SMILES
[C@@H](N[C@H]1C[C@@H](C(O)=O)C1)(C)C2=CC=C(C=3N=C(ON3)C4=CC=C(CC(C)C)C=C4)C=C2
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Synonyms
PF-991
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Horan JC, et al. Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists. Bioorg Med Chem Lett. 2016;26(2):466-471. [Content Brief]
[2]. Dyckman AJ, et al. Modulators of Sphingosine-1-phosphate Pathway Biology: Recent Advances of Sphingosine-1-phosphate Receptor 1 (S1P1) Agonists and Future Perspectives. J Med Chem. 2017;60(13):5267-5289. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PF-462991 Related Classifications
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