RO 46-8443

• CAT Number: I009150
• CAS Number: 175556-12-4
• Molecular Formula: C31H35N3O8S
• Molecular Weight: 609.694
• Purity: ≥95%
• Synonyms: RO 46-8443; RO46-8443; RO-46-8443; RO 468443; RO-468443; RO468443; RO 46,8443; RO-46,8443; RO46,8443.;4-(tert-butyl)-N-(6-(2,3-dihydroxypropoxy)-5-(2-methoxyphenoxy)-2-(4-methoxyphenyl)pyrimidin-4-yl)benzenesulfonamide
• Target: Endothelin Receptor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• IUPAC Name: 4-tert-butyl-N-[6-(2,3-dihydroxypropoxy)-5-(2-methoxyphenoxy)-2-(4-methoxyphenyl)pyrimidin-4-yl]benzenesulfonamide
• InChI: InChI=1S/C31H35N3O8S/c1-31(2,3)21-12-16-24(17-13-21)43(37,38)34-29-27(42-26-9-7-6-8-25(26)40-5)30(41-19-22(36)18-35)33-28(32-29)20-10-14-23(39-4)15-11-20/h6-17,22,35-36H,18-19H2,1-5H3,(H,32,33,34)
• InChIKey: DRIHNVYRUGBDHI-UHFFFAOYSA-N
• SMILES: CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=CC=C(C=C3)OC)OCC(CO)O)OC4=CC=CC=C4OC

RO 46-8443(CAT: I009150) is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors in terms of binding inhibitory potency and functional inhibition. The observed parallel rightward shift of concentration-response curves with different antagonist concentrations is consistent with a competitive compulsory mode. Since R0 46-8443 selectively inhibits ETB receptor-mediated responses, it is a valuable tool for clarifying the role of ETB receptors in pathology.

Reference

1:The role of ETB receptors in normotensive and hypertensive rats as revealed by the non-peptide selective ETB receptor antagonist Ro 46-8443. Clozel M, Breu V.FEBS Lett. 1996 Mar 25;383(1-2):42-5. PMID: 8612787 Free Article2:In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ETB receptor. Breu V, Clozel M, Burri K, Hirth G, Neidhart W, Ramuz H.FEBS Lett. 1996 Mar 25;383(1-2):37-41. PMID: 8612786 Free Article