Ex 26

Tocris Bioscience, part of Bio-Techne | Catalog # 5833

COA / SDS

Potent and selective S1P1 receptor antagonist

Key Product Details

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)
Molecular Weight:	494.98

View Full Technical Details for Ex 26

Technical Data
Citations

Biological Activity for Ex 26

Ex 26 is a 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.

Compound Libraries for Ex 26

Ex 26 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Ex 26

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 for Ex 26

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

Preparing Stock Solutions for Ex 26

The following data is based on the product molecular weight 494.98.

Batch specific molecular weights may vary from batch to batch due to the degree 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	10.10 mL	20.20 mL
5 mM	0.40 mL	2.02 mL	4.04 mL
10 mM	0.20 mL	1.01 mL	2.02 mL
50 mM	0.04 mL	0.20 mL	0.40 mL

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References for Ex 26

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

Cahalan Sphingosine 1-phosphate receptor 1 (S1P₁) upregulation and amelioration of experimental autoimmune encephalomyelitis by an S1P₁ antagonist. Mol.Pharmacol. 2013 PMID: 23204443
Kleinwort S1P signalling differentially affects migration of peritoneal B cell populations in vitro and influences the production of intestinal IgA in vivo. Int.J.Mol.Sci. 2018 PMID: 29382132
Teijaro S1PR₁-mediated IFNAR1 degradation modulates plasmacytoid dendritic cell IF.-a autoamplification. Proc.Natl.Acad.Sci.U.S.A. 2016 PMID: 26787880