S-(+)-PD 123177 trifluoroacetate salt hydrate

• Catalog No.: P5749
• M. F.: C31H31F3N4O6
• M. W.: 612.5962496
• Purity: ≥98% (HPLC)

SYNONYMS

• IUPAC name: (6S)-1-[(4-amino-3-methylphenyl)methyl]-5-(2,2-diphenylacetyl)-1H,4H,5H,6H,7H-imidazo[4,5-c]pyridine-6-carboxylic acid trifluoroacetic acid hydrate
• IUPAC Traditional name: (6S)-1-[(4-amino-3-methylphenyl)methyl]-5-(2,2-diphenylacetyl)-4H,6H,7H-imidazo[4,5-c]pyridine-6-carboxylic acid trifluoroacetic acid hydrate
• Synonyms: (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

DATABASE IDS

• MDL Number: MFCD09265257
• PubChem SID: 24724581

PROPERTIES

• Empirical Formula (Hill Notation): C29H28N4O3 · xC2HF3O2 · yH2O
• Purity: ≥98% (HPLC)
• Apperance: white to off-white solid
• Solubility: H2O: >5 mg/mL
• Storage Temperature: 2-8°C
• German water hazard class: 3

DETAILS

Description (English)

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.

Description (简体中文)

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.