AMG-548
Cat. No.:YN350057
产品名称: | AMG-548 |
CAS No.: | 864249-60-5 |
Chemical Name: | 2-[[(2S)-2-amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone |
Synonyms: | AMG548;AMG 548 |
分子量: | 461.56 |
分子式: | C₂₉H₂₇N₅O |
SMILES: | O=C1N(C)C(NC[C@@H](N)CC2=CC=CC=C2)=NC(C3=CC=NC=C3)=C1C4=CC=C5C=CC=CC5=C4 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | AMG-548 是一种口服有效的,选择性p38α抑制剂 (Ki=0.5 nM),对p38β略有选择性 (Ki=36 nM) 并且对 p38γ 和 p38δ 具有 >1000 倍的选择性。AMG 548 也有效抑制全血 LPS 刺激的TNFα(IC50=3 nM)。AMG-548 通过直接抑制酪蛋白激酶 1 (Casein kinase 1) 同种型 δ 和 ε 来抑制 Wnt 信号传导。 |
IC50和靶点: | [{name:"p38α:0.5 nM (Ki)"},{name: "p38β:3.6 nM (Ki)"},{name: "p38δ:2600 nM (Ki)"},{name: "p38γ:4100 nM (Ki)"},{name: "dog p38α:5.0 nM (Ki)"},{name: "JNK1:11480 nM (Ki)"},{name: "JNK2:39 nM (Ki)"},{name: "JNK3:61 nM (Ki)'}, 'CK1'] |
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Solvent & Solubility: |
Lee, M.R., and Dominguez, C.MAP kinase p38 inhibitors: Clinical results and an intimate look at their interactions with p38α proteinCurr. Med. Chem.12(25),2979-2994(2005)