S-(+)-PD 123177 trifluoroacetate salt MF: C29H28N4O3•xC2HO2F3

S-(+)-PD 123177 trifluoroacetate salt

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备用名: (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
纯度: ≥98%
分子式: C29H28N4O3•xC2HO2F3
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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S-(+)-PD 123177 trifluoroacetate salt is a 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. 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.


参考文献

1. Olivares-Reyes, J.A., et al. 2000. Mol. Pharmacol. 58: 1156-1161. PMID: 11040065

物理状态 :
Solid
溶解度 :
Soluble in water (>5 mg/ml).
保存 :
Store at 4° C
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
MDL 号码 :
MFCD09265257

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