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P5749 Sigma-Aldrich

S-(+)-PD 123177 trifluoroacetate salt hydrate

≥98% (HPLC), solid

Synonym: (S)-1-[(4-Amino-3-methylphenyl)methyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-Imidazo[4,5-c]pyridine-6-carboxylic acid trifluoroacetate salt hydrate

  • Empirical Formula (Hill Notation) C29H28N4O3 · xC2HF3O2 · yH2O

  • Molecular Weight 480.56 (anhydrous free base basis)

  •  MDL number MFCD09265257

  •  PubChem Substance ID 24724581

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Description

Packaging

10 mg in glass bottle

Biochem/physiol Actions

S-(+)-PD 123177 is selective AT2 angiotensin receptor antagonist. The angiotensin AT2 receptor is an atypical seven transmembrane domain receptor that is coupled to activation of tyrosine phosphatase and inhibition of MAP kinase, and does not undergo agonist-induced internalization. An investigation of the occurrence and nature of AT2 receptor phosphorylation revealed that phorbol ester-induced activation of protein kinase C (PKC) in HA-AT2 receptor-expressing COS-7 cells caused rapid and specific phosphorylation of a single residue (Ser354) located in the cytoplasmic tail of the receptor. Agonist activation of AT2 receptors by angiotensin II (Ang II) also caused rapid PKC-dependent phosphorylation of Ser354 that was prevented by the AT2 antagonist, S-(+)-PD 123177, and by inhibitors of PKC. In cells coexpressing AT1 and AT2 receptors, Ang II-induced phosphorylation of the AT2 receptor was reduced by S-(+)-PD 123177 and abolished by treatment with both antagonists or with PKC inhibitors. These findings indicate that the AT2 receptor is rapidly phosphorylated via PKC during homologous activation by Ang II, and also undergoes heterologous PKC-dependent phosphorylation during activation of the AT1 receptor.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is featured on the Angiotensin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Pfizer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

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Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis


Making Headway

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Protocols & Articles

Articles

Angiotensin Receptors

Different receptors/binding sites have been identified for the biologically active angiotensin (Ang) peptides, i.e. Ang II (1-8), Ang III (2-8), Ang IV (3-8) and Ang (1-7), based on the availability ...
Keywords: Atomic absorption spectroscopy, Cardiovascular, Catalysis, Cell proliferation, Gene expression, Ligands, Metabolites, Transduction

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