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

CAY10535 Exclusive

Cayman Chemical Item Number 10010396

CAY10535

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Description

TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC50 = 99 nM) relative to TPα (IC50 = 1,970 nM) in the inhibition of U-46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.1

1 Hanson, J., Dogné, J., Ghiotto, J., et al. Design, synthesis, and SAR study of a series of N-alkyl-N'-[2-(aryloxy)-5-nitrobenzenesulfonyl]ureas and -cyanoguanidine as selective antagonists of the TPα and TPβ isoforms of the human thromboxane A2 receptor. J Med Chem 50(16) 3928-3936 (2007).

Formal Name N-​(tert-​butylcarbamoyl)-​2-​(3-​methoxyphenoxy)-​5-​nitrobenzenesulfonamide
Molecular Formula C18H21N3O7S
Formula Weight 423.4
Formulation A crystalline solid
Purity >98%
λmax 294 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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COc1cccc(c1)​Oc1ccc(cc1S(=O)​(=O)​NC(=O)​NC(C)​(C)​C)​[N]​(=O)​O

Background Reading

Hanson, J., Dogné, J., Ghiotto, J., et al. Design, synthesis, and SAR study of a series of N-alkyl-N'-[2-(aryloxy)-5-nitrobenzenesulfonyl]ureas and -cyanoguanidine as selective antagonists of the TPα and TPβ isoforms of the human thromboxane A2 receptor. J Med Chem 50(16) 3928-3936 (2007).
Size Price Quantity Subtotal
1 mg $36.00 $0.00
5 mg $162.00 $0.00
10 mg $288.00 $0.00
50 mg $1,260.00 $0.00
Bulk Contact
Cart Total $0.00

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

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Warning This product is not for human or veterinary use.

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U-46619

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