CAS NO: | 261766-29-4 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 433.9 |
Cas No. | 261766-29-4 |
Formula | C24H20ClN3O3 |
Synonyms | N-3PyIA |
Solubility | ≤3mg/ml in ethanol;3mg/ml in DMSO;3mg/ml in dimethyl formamide |
Chemical Name | N-(3-pyridyl)-1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetamide |
Canonical SMILES | ClC1=CC=C(C(N2C(C=CC(OC)=C3)=C3C(CC(N([H])C4=CN=CC=C4)=O)=C2C)=O)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
N-(3-pyridyl)-Indomethacin amide is a reversible, potent and selective COX-2 inhibitor [1].
Cyclooxygenase (COX) is an enzyme responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. COX-1 is the constitutive isoform and is mainly responsible for the synthesis of cytoprotective prostaglandins in the gastrointestinal tract (GI) and of the proaggregatory thromboxane in blood platelets. COX-2 is inducible and short-lived that is stimulated by endotoxin, cytokines, and mitogens. COX-2 plays important roles in prostaglandin biosynthesis in inflammatory cells the central nervous system [1].
N-(3-pyridyl)-indomethacin amide (N-3PyIA) is a reversible, potent and selective COX-2 inhibitor that inhibits human recombinant COX-2 and ovine COX-1 with IC50 values of 0.052 and >66 μM, respectively. It is over 1300 times less potent as an inhibitor of ovine COX-1. N-(3-pyridyl)-indomethacin amide is the 3-pyridyl amide derivative of indomethacin that shows selective against COX-2 [1].
Reference:
[1]. Kalgutkar AS, Marnett AB, Crews BC, et al. Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. J Med Chem. 2000 Jul 27;43(15):2860-70.