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Cat. No.: HY-14433

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PF-462991

(Synonyms: PF-991)

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.

For research use only. We do not sell to patients.

CAS No.: 1149727-90-1
Formula: C₂₅H₂₉N₃O₃
Molecular Weight:419.53

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PF-462991 Chemical Structure

CAS No.: 1149727-90-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

S1PR1

1.9 nM (EC₅₀)

All LPL Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
U2OS	EC₅₀	>10 μM 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]
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]

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.

Chemical Information

CAS No. 1149727-90-1
Molecular Weight 419.53
Formula C₂₅H₂₉N₃O₃
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
Synonyms

PF-991
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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