S-(+)-PD 123177 trifluoroacetate salt hydrate P5749-10MG

Empirical Formula (Hill Notation):	C29H28N4O3 · xC2HF3O2 · yH2O
Molecular Weight:	480.56 (anhydrous free base basis)
MDL number:	MFCD09265257
PubChem Substance ID:	24724581
NACRES:	NA.77

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 was developed by Pfizer,. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here,.
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,.
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Quality Level	100,
assay	98% (HPLC)
form	solid
color	white to off-white
solubility	H2O: >5 mg/mL
originator	Pfizer
storage temp.	2-8°C
SMILES string	O.OC(=O)C(F)(F)F.Cc1cc(Cn2cnc3CN([C@@H](Cc23)C(O)=O)C(=O)C(c4ccccc4)c5ccccc5)ccc1N
InChI	1S/C29H28N4O3.C2HF3O2.H2O/c1-19-14-20(12-13-23(19)30)16-32-18-31-24-17-33(26(29(35)36)15-25(24)32)28(34)27(21-8-4-2-5-9-21)22-10-6-3-7-11-22;3-2(4,5)1(6)7;/h2-14,18,26-27H,15-17,30H2,1H3,(H,35,36);(H,6,7);1H2/t26-;;/m0../s1
InChI key	IRRZMYRIDIBBQG-ROPHLPQBSA-N

RIDADR	NONH for all modes of transport
WGK Germany	WGK 3
Flash Point F	Not applicable
Flash Point C	Not applicable