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Submit ReviewTASP 0277308
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)
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 |
| InChI Key | MVOULGOLHZCXLD-MRXNPFEDSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for TASP 0277308
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
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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
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