P5749

S-(+)-PD 123177 trifluoroacetate salt hydrate

≥98% (HPLC), solid

• 동의어(들): (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
• 실험식(Hill 표기법): C₂₉H₂₈N₄O₃ · xC₂HF₃O₂ · yH₂O
• Molecular Weight: 480.56 (anhydrous free base basis)
• MDL number: MFCD09265257
• UNSPSC 코드: 12352200
• PubChem Substance ID: 24724581
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: solid
• 색상: white to off-white
• solubility: H₂O: >5 mg/mL
• 저장 온도: 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

설명

생화학적/생리학적 작용

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 Ser^{354 t}hat 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.

특징 및 장점

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.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable