N-(3-PYRIDYL)-INDOMETHACIN AMIDE
N-(3-PYRIDYL)-INDOMETHACIN AMIDE Basic information
- Product Name:
- N-(3-PYRIDYL)-INDOMETHACIN AMIDE
- Synonyms:
-
- N-(3-PYRIDYL)-1-(4-CHLOROBENZOYL)-5-METHOXY-2-METHYL-1H-INDOLE-3-ACETAMIDE
- N-(3-PYRIDYL)-1-P-CHLOROBENZOYL-5-METHOXY-2-METHYLINDOLE-3-ACETAMIDE
- N-(3-PYRIDYL)-INDOMETHACIN AMIDE
- N-3PYIA
- N-3PyIA, N-(3-Pyridyl)-1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetamide
- 1-(4-Chlorobenzoyl)-5-Methoxy-2-Methyl-N-3-pyridinyl-1H-indole-3-acetaMide
- 2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]-N-pyridin-3-ylacetamide
- Indomethacin N-Pyridyl Impurity
- CAS:
- 261766-29-4
- MF:
- C24H20ClN3O3
- MW:
- 433.89
- Product Categories:
-
- Inhibitors
- Mol File:
- Mol File
N-(3-PYRIDYL)-INDOMETHACIN AMIDE Chemical Properties
- storage temp.
- −20°C
- solubility
- ≤3mg/ml in ethanol;3mg/ml in DMSO;3mg/ml in dimethyl formamide
- form
- crystalline solid
MSDS
- Language:English Provider:SigmaAldrich
N-(3-PYRIDYL)-INDOMETHACIN AMIDE Usage And Synthesis
Uses
An aromatic amide of indomethacin recently reported to be a potent and selective reversible inhibitor of COX-2. Inhibits human recombinant COX-2 with IC50 of 0.1 uM.
Biological Activity
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].
References
[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.
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