APD668
Cat. No.：YN321006
CAS No. ：832714-46-2
| 产品名称: | APD668 |
| CAS No.: | 832714-46-2 |
| Chemical Name: | 4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-1-piperidinecarboxylic acid, 1-methylethyl ester |
| Synonyms: | JNJ28630368 |
| 分子量: | 477.51 |
| 分子式: | C₂₁H₂₄FN₅O₅S |
| SMILES: | O=C(OC(C)C)N(CC1)CCC1OC2=C3C(N(C4=CC=C(S(=O)(C)=O)C=C4F)N=C3)=NC=N2 |
| 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: | APD668 是一种有效的，选择性和具有口服活性的 G 蛋白偶联受体GPR119激动剂，对hGPR119和rGPR119的EC50值分别为 2.7 nM 和 33 nM。APD668 对除CYP2C9(Ki=0.1 μM) 以外的五种主要 CYP 亚型均无明显抑制作用。APD668 可用于脂肪性肝炎和糖尿病的研究。 |
| IC50和靶点: | [{name:"CYP2C9:0.1 μM (Ki)"},{name: "hGPR119:2.7 nM (IC50)"},{name: "rGPR119:33 nM (IC50)"},{name: "hERG channel:3 μM (IC50)"}] |
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Overton, H.A., Babbs, A.J., Doel, S.M., et al.Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agentsCell Metab.3(3),167-175(2006)
Soga, T., Ohishi, T., Matsui, T., et al.Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptorBiochem. Biophys. Res. Commun.326(4),744-751(2005)
Semple, G., Ren, A., Fioravanti, B., et al.Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose controlBioorg. Med. Chem. Lett.21(10),3134-3141(2011)
