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S-(+)-PD 123177 trifluoroacetate salt hydrate,≥98% (HPLC), solid

别名:S-(+)-PD 123177三氟乙酸盐水合物;PD-123177;PD123177;(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 分子量: 480.56 (anhydrous free base basis) MDL编号: MFCD09265257 PubChem化学物质编号: 24724581 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): P5749
MDL号: MFCD09265257
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$927.57

说明

包装

10 mg in glass bottle
 

生化/生理作用

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.
 
S-(+)-PD 123177 是选择性 AT2 血管紧张素受体拮抗剂。血管紧张素 AT2 受体是一种非典型的七跨膜结构域受体,它与酪氨酸磷酸酶的激活和 MAP 激酶的抑制相结合,并且不经历激动剂诱导的内化。对 AT2 受体磷酸化的发生和性质的研究表明,在表达 HA-AT2 受体的 COS-7 细胞中,佛波酯诱导的蛋白激酶 C (PKC) 激活导致位于 HA-AT2 受体的单个残基 (Ser354) 的快速和特异性磷酸化。受体的细胞质尾部。血管紧张素 II (Ang II) 对 AT2 受体的激动剂激活也引起了 Ser354 的快速 PKC 依赖性磷酸化,这被 AT2 拮抗剂 S-(+)-PD 123177 和 PKC 抑制剂阻止。在共表达 AT1 和 AT2 受体的细胞中,Ang II 诱导的 AT2 受体磷酸化被 S-(+)-PD 123177 降低,并被两种拮抗剂或 PKC 抑制剂治疗消除。这些发现表明 AT2 受体在 Ang II 同源激活期间通过 PKC 快速磷酸化,并且在 AT1 受体激活期间也经历异源 PKC 依赖性磷酸化。
 

特点和优势

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 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.
 

法律信息

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC
 

属性

质量水平

100

测定

≥98% (HPLC)

形式

solid

颜色

white to off-white

溶解性

H2O: >5 mg/mL

创始人

Pfizer

储存温度

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

 

安全信息

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16