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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- No. CAS: 1149727-90-1
- Fòrmula: C25H29N3O3
- Peso molecular:419.53
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
IC50 & Target
[1]|
S1PR1 1.9 nM (EC50) |
Cellular Effect
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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
|
[PMID: 26687487] |
| U2OS | EC50 |
1.9 nM
Compound: PF-991
|
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
|
[PMID: 26687487] |
| U2OS | EC50 |
10000 nM
Compound: PF-991
|
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
|
[PMID: 26687487] |
In Vitro
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. Further protocols information, click here.
Chemical Information
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No. CAS 1149727-90-1
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Peso molecular 419.53
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)