JTE-013 is a potent

JTE-013 – 10 mg

Brand:
Cayman
CAS:
383150-41-2
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} JTE-013 is a potent, selective sphingosine-1-phosphate 2 (S1P2) receptor antagonist that binds to the human and rat receptors with IC50 values of 17 and 22 nM, respectively, (IC50 values >10 µM for human S1P1 and S1P3).{14560} It reverses the inhibitory effects of S1P on cell migration of vascular endothelial cells and smooth muscle cells. Similarly, JTE-013 reverses the inhibition of S1P on invasion and migration of B16 melanoma cells.{14560,14559} JTE-013 inhibits S1P-induced contraction of, as well as cyclic AMP accumulation in, coronary artery smooth muscle cells.{14558,14556}  

 

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SKU: 10009458 - 10 mg Category:

Description

JTE-013 is a potent, selective S1P2 receptor antagonist that binds to the human and rat receptors with IC50 values of 17 and 22 nM, respectively, (IC50 values >10 µM for human S1P1 and S1P3).{14560} It reverses the inhibitory effects of S1P on cell migration of vascular endothelial cells and smooth muscle cells. Similarly, JTE-013 reverses the inhibition of S1P on invasion and migration of B16 melanoma cells.{14560,14559} JTE-013 inhibits S1P-induced contraction of, as well as cAMP accumulation in, coronary artery smooth muscle cells.{14558,14556}

Formal name: N-(2,6-dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-hydrazinecarboxamide

Synonyms: 

Molecular weight: 408.3

CAS: 383150-41-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cardiovascular System|Vasculature|Endothelium||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Cell Biology|Cell Signaling|cAMP Signaling||Research Area|Lipid Biochemistry|Sphingolipids

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