JTE 013 | Sphingosine-1-phosphate Receptors | S1P2 Receptor Antagonist | JTE013

Category:

Cat.No.	Product Name
2392	JTE 013

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JTE 013

Chemical Name: 1-[1,3-Dimethyl-4-(2-methylethyl)-1H-pyrazolo[3,4-b]pyr idin-6-yl]-4-(3,5-dichloro-4-pyridinyl)-semicarbazide

Biological Activity:

Sphingosine-1-phosphate (S1P) receptor antagonist, highly selective for S1P₂ (EDG-5). Inhibits S1P binding to human S1P₂ receptors with an IC₅₀ value of 17.6 nM. At concentrations up to 10 μM, displays 4.2% inhibition of S1P₃ and does not antagonise S1P₁. Enhances S1P-induced angiogenesis in vivo.

Technical Data:

M.Wt:	408.29
Formula:	C₁₇H₁₉N₇OCl₂
Storage:	Store at +4°C
Solubility:	Soluble to 100 mM in DMSO and to 100 mM in Ethanol
Purity:	>98%
CAS No:	[547756-93-4]

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References:

Ohmori et al (2003) Spingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P₂. Cardiovasc.Res. 58 170. Parrill et al (2004) Sphingosine 1-phosphate and lysophosphatidic acid receptors: agonist and antagonist binding and progress toward development of receptor-specific ligands. Semin.Cell.Dev.Biol. 15 467. Inoki et al (2006) Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor. Biochem.Biophys.Res.Comm. 346 293.

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Keywords: JTE 013, Sphingosine-1-phosphate Receptors, S1P2 Receptor Antagonist, JTE013, Tocris Bioscience

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