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RO 46-8443

  Cat. No.:  DC33038   Featured
Chemical Structure
175556-12-4
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Field of application
RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both 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 binding 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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 175556-12-4
Chemical Name: 4-(tert-butyl)-N-(6-(2,3-dihydroxypropoxy)-5-(2-methoxyphenoxy)-2-(4-methoxyphenyl)pyrimidin-4-yl)benzenesulfonamide
Synonyms: RO 46-8443; RO46-8443; RO-46-8443; RO 468443; RO-468443; RO468443; RO 46,8443; RO-46,8443; RO46,8443.
SMILES: COC(C=CC=C1)=C1OC2=C(OCC(O)CO)N=C(C3=CC=C(OC)C=C3)N=C2NS(C4=CC=C(C(C)(C)C)C=C4)(=O)=O
Formula: C31H35N3O8S
M.Wt: 609.694
Purity: >98%
Sotrage: -20
Description: RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both 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 binding 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.
Target: ETB:34-69 nM (IC50) ETA:6800 nM (IC50)
References: [1]. Breu V, et al. In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ETB receptor. FEBS Lett. 1996;383(1-2):37-41. [2]. Clozel M, et al. The role of ETB receptors in normotensive and hypertensive rats as revealed by the non-peptide selective ETB receptor antagonist Ro 46-8443. FEBS Lett. 1996;383(1-2):42-45.
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