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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

JTE-013

Cayman Chemical Item Number 10009458

(CAS 383150-41-2)

JTE-013 (CAS 383150-41-2)

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Cayman and its customers are licensed to make, have made, sell and use the polynucleotides encoding the S1P2 (Sphingosine 1-Phosphate Receptor 2/ aka Edg 5/ aka PH218) receptor, complementary polynucleotides, and polypeptides and all matter claimed in U.S. Patent No. 5,585,476, U.S. Patent No. 5,856,443, and U.S. Patent No. 6,518,414B1. THIS LICENSE DOES NOT EXTEND TO THE MANUFACTURE AND SALE OF ANY DRUG PRODUCT. Notwithstanding any express or implied warranties to the contrary, including but not limited to Uniform Commercial Code § 2-312(3), Cayman expressly disclaims any and all liability for any claims arising out of or relating to the manufacture and sale of drug products using polynucleotides encoding the S1P2 (Sphingosine 1-Phosphate Receptor 2/ aka Edg 5/ aka PH218) receptor, complementary polynucleotides, and polypeptides or any matter claimed in U.S. Patent No. 5,585,476, U.S. Patent No. 5,856,443, and U.S. Patent No. 6,518,414B1.

Description

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.1,2,3 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-8.1,2 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).4 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.4,5 JTE-013 inhibits S1P-induced contraction of, as well as cyclic AMP accumulation in, coronary artery smooth muscle cells.6,7

1 Takuwa, Y., Takuwa, N., and Sugimoto, N. The Edg family G protein-coupled receptors for lysophospholipids: Their signaling properties and biological activities. J Biochem 131 767-771 (2002).

2 Ishii, I., Fukushima, N., Ye, X., et al. Lysophospholipid receptors: Signaling and biology. Annu Rev Biochem 73 321-354 (2004).

3 Kluk, M.J., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim Biophys Acta 1582 72-80 (2002).

4 Osada, M., Yatomi, Y., Ohmori, T., et al. Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist. Biochem Biophys Res Commun 299 483-487 (2002).

5 Arikawa, K., Takuwa, N., Yamaguchi, H., et al. Ligand-dependent inhibition of B16 melanoma cell migration and invasion via endogenous S1P2 G protein-coupled receptor. Requirement of inhibition of cellular rac activity. J Biol Chem 278(35) 32841-32851 (2003).

6 Damirin, A., Tomura, H., Komachi, M., et al. Sphingosine 1-phosphate receptors mediate the lipid-induced cAMP accumulation through cyclooxygenase-2/prostaglandin I2 pathway in human coronary artery smooth muscle cells. Mol Pharmacol 67(4) 1177-1185 (2005).

7 Ohmori, T., Yatomi, Y., Osada, M., et al. Sphingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2. Cardiovasc Res 58 170-177 (2003).

Formal Name N-​(2,​6-​dichloro-​4-​pyridinyl)-​2-​[1,​3-​dimethyl-​4-​(1-​methylethyl)-​1H-​pyrazolo[3,​4-​b]pyridin-​6-​yl]-​hydrazinecarboxamide
CAS Number 383150-41-2
Molecular Formula C17H19Cl2N7O
Formula Weight 408.3
Formulation A crystalline solid
Purity ≥98%
λmax 216, 248, 304 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
Copy SMILES to clipboard
O=C(NNc1cc(C(C)​C)​c2c(C)​nn(C)​c2n1)​Nc1cc(Cl)​nc(Cl)​c1

Background Reading

Takuwa, Y., Takuwa, N., and Sugimoto, N. The Edg family G protein-coupled receptors for lysophospholipids: Their signaling properties and biological activities. J Biochem 131 767-771 (2002).

Kluk, M.J., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim Biophys Acta 1582 72-80 (2002).

Ishii, I., Fukushima, N., Ye, X., et al. Lysophospholipid receptors: Signaling and biology. Annu Rev Biochem 73 321-354 (2004).

Osada, M., Yatomi, Y., Ohmori, T., et al. Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist. Biochem Biophys Res Commun 299 483-487 (2002).

Damirin, A., Tomura, H., Komachi, M., et al. Sphingosine 1-phosphate receptors mediate the lipid-induced cAMP accumulation through cyclooxygenase-2/prostaglandin I2 pathway in human coronary artery smooth muscle cells. Mol Pharmacol 67(4) 1177-1185 (2005).

Ohmori, T., Yatomi, Y., Osada, M., et al. Sphingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2. Cardiovasc Res 58 170-177 (2003).

Arikawa, K., Takuwa, N., Yamaguchi, H., et al. Ligand-dependent inhibition of B16 melanoma cell migration and invasion via endogenous S1P2 G protein-coupled receptor. Requirement of inhibition of cellular rac activity. J Biol Chem 278(35) 32841-32851 (2003).

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JTE-013 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $19.00 $0.00
5 mg $86.00 $0.00
10 mg $152.00 $0.00
50 mg $665.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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Cayman and its customers are licensed to make, have made, sell and use the polynucleotides encoding the S1P2 (Sphingosine 1-Phosphate Receptor 2/ aka Edg 5/ aka PH218) receptor, complementary polynucleotides, and polypeptides and all matter claimed in U.S. Patent No. 5,585,476, U.S. Patent No. 5,856,443, and U.S. Patent No. 6,518,414B1. THIS LICENSE DOES NOT EXTEND TO THE MANUFACTURE AND SALE OF ANY DRUG PRODUCT. Notwithstanding any express or implied warranties to the contrary, including but not limited to Uniform Commercial Code § 2-312(3), Cayman expressly disclaims any and all liability for any claims arising out of or relating to the manufacture and sale of drug products using polynucleotides encoding the S1P2 (Sphingosine 1-Phosphate Receptor 2/ aka Edg 5/ aka PH218) receptor, complementary polynucleotides, and polypeptides or any matter claimed in U.S. Patent No. 5,585,476, U.S. Patent No. 5,856,443, and U.S. Patent No. 6,518,414B1.

Cayman Chemical is a manufacturer, supplier and vendor of biochemical reagents, assay kits, antibodies, and proteins.

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