TASP 0277308

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Description: Potent and selective S1P1 receptor antagonist; inhibits angiogenesis
Chemical Name: 3,4-Dichloro-N-[(1R)-1-[4-ethyl-5-[3-(4-methyl-1-piperazinyl)phenoxy]-4H-1,2,4-triazol-3-yl]ethyl]benzenesulfonamide
Purity: ≥98% (HPLC)
Literature (3)

Biological Activity for TASP 0277308

TASP 0277308 is a potent and selective sphingosine 1-phosphate 1 (S1P1) receptor antagonist (IC50 = 7.8 nM). TASP 0277308 inhibits S1P-induced chemotaxis (IC50 = 1.1-1.6 nM), HUVEC cell proliferation (IC50 = 3-3.6 nM) and suppresses angiogenesis in vivo. TASP 0277308 also blocks VEGF-induced tube-formation of HUVECs in vitro and reverses or impairs the development of arthritis or mechano-allodynia.

Technical Data for TASP 0277308

M. Wt 539.48
Formula C23H28Cl2N6O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 945725-50-8
PubChem ID 56935569
Smiles CCN1C(OC2=CC(N3CCN(CC3)C)=CC=C2)=NN=C1[C@H](NS(=O)(C4=CC(Cl)=C(C=C4)Cl)=O)C

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 for TASP 0277308

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 2.7 5

Preparing Stock Solutions for TASP 0277308

The following data is based on the product molecular weight 539.48. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 37.07 mL 185.36 mL 370.73 mL
0.25 mM 7.41 mL 37.07 mL 74.15 mL
0.5 mM 3.71 mL 18.54 mL 37.07 mL
2.5 mM 0.74 mL 3.71 mL 7.41 mL

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References for TASP 0277308

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

Fujii et al (2012) Amelioration of collagen-induced arthritis by a novel S1P1 antagonist with immunomodulatory activities. J.Immunol. 188 PMID: 22131329

Fujii et al (2012) Blocking S1P interaction with S1P1 receptor by a novel competitive S1P1-selective antagonist inhibits angiogenesis. Biochem.Biophys.Res.Commun. 419 754 PMID: 22387544

If you know of a relevant reference for TASP 0277308, please let us know.

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Keywords: TASP 0277308, TASP 0277308 supplier, TASP0277308, potent, selective, sphingosine, 1-phosphate, antagonists, S1P1-receptors, Sphingosine-1-phosphate, Receptors, Antiangiogenics, 6498, Tocris Bioscience

Citations for TASP 0277308

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