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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1149727-90-1
- 分子式: C25H29N3O3
- 分子量:419.53
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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
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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
|
[PMID: 26687487] |
| U2OS | EC50 |
10000 nM
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] |
体外実験
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.
化学情報
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CAS 番号 1149727-90-1
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分子量 419.53
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分子式 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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別名
PF-991
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PF-462991 関連分類
HY-14433 関連分類
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