Ex 26

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Cat.No. 5833 - Ex 26 | C28H28ClFN2O3 | CAS No. 1233332-37-0
Description: Potent and selective S1P1 receptor antagonist
Chemical Name: 1-[[[5'-[[1-(4-Chloro-3-methylphenyl)ethyl]amino]-2'-fluoro-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]amino]-cyclopropanecarboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective S1P1 receptor antagonist (IC50 = 0.93 nM). Exhibits > 3,000-fold selectivity for S1P1 over S1P2, S1P3, S1P4 and S1P5. Induces lymphocyte sequestration in peripheral lymph nodes and upregulates S1P1 receptor expression. Reduces disease severity in mice with EAE. Increases IFN-α production in stimulated dendritic cells in vivo.

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Technical Data

M. Wt 494.98
Formula C28H28ClFN2O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1233332-37-0
PubChem ID 59393740
InChI Key YVHNBORUVLWCKF-UHFFFAOYSA-N
Smiles CC(C1=CC(C)=C(C=C1)Cl)NC2=CC=C(C(C3=CC(C)=C(C(C)=C3)C(NC4(C(O)=O)CC4)=O)=C2)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.5 100
ethanol 49.5 100

Preparing Stock Solutions

The following data is based on the product molecular weight 494.98. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.02 mL 10.1 mL 20.2 mL
5 mM 0.4 mL 2.02 mL 4.04 mL
10 mM 0.2 mL 1.01 mL 2.02 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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References

References are publications that support the biological activity of the product.

Teijaro et al (2016) S1PR1-mediated IFNAR1 degradation modulates plasmacytoid dendritic cell interferon-a autoamplification. Proc.Natl.Acad.Sci.U.S.A. 113 1351 PMID: 26787880

Cahalan et al (2013) Sphingosine 1-phosphate receptor 1 (S1P1) upregulation and amelioration of experimental autoimmune encephalomyelitis by an S1P1 antagonist. Mol.Pharmacol. 83 316 PMID: 23204443


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Keywords: Ex 26, Ex 26 supplier, Ex26, sphingosine-1-phosphate, S1P1, S1P1R, antagonists, antagonism, selective, Sphingosine-1-phosphate, Receptors, 5833, Tocris Bioscience

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