N-(2-PHENYLETHYL)-INDOMETHACIN AMIDE
- CAS NO.:261766-32-9
- Empirical Formula: C27H25ClN2O3
- Molecular Weight: 460.95
- MDL number: MFCD02683391
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-05-18 11:31:03
What is N-(2-PHENYLETHYL)-INDOMETHACIN AMIDE?
The Uses of N-(2-PHENYLETHYL)-INDOMETHACIN AMIDE
An aromatic amide of indomethacin recently reported to be a potent and selective reversible inhibitor of COX-2. Inhibits human recombinant and ovine COX-2 with IC50 of 0.06 uM and 0.125 uM, respectively
The Uses of N-(2-PHENYLETHYL)-INDOMETHACIN AMIDE
N-(2-Phenylethyl)indomethacin Amide is an aromatic amide of indomethacin reported to be a potent and selective reversible inhibitor of COX-2. N-(2-Phenylethyl)indomethacin Amide inhibits human recombinant and ovine COX-2 with IC50 of 0.06 uM and 0.125 uM, respectively.
What are the applications of Application
N-(2-Phenylethyl)indomethacin Amide is an inhibitor of Cox-2
Definition
ChEBI: N-(2-phenylethyl)-Indomethacin amide is a N-acylindole.
Biological Activity
n-(2-phenylethyl)-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-(2-phenylethyl)-indomethacin amide (n-2pia) is a reversible, potent and selective cox-2 inhibitor that inhibits human recombinant cox-2 and ovine cox-1 with ic50 values of 0.06 and >66 μm, respectively. it is over 1000 times less potent as an inhibitor of ovine cox-1. n-(2-phenylethyl)-indomethacin amide is an analogous derivative of indomethacin that shows selective against cox-2 [1].in the carageenan-induced foot pad edema assay, orally administration of n-2pia showed anti-inflammatory activity [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.
Properties of N-(2-PHENYLETHYL)-INDOMETHACIN AMIDE
Boiling point: | 640.5±55.0 °C(Predicted) |
Density | 1.22±0.1 g/cm3(Predicted) |
storage temp. | −20°C |
solubility | ≤80mg/ml in ethanol;10mg/ml in DMSO;14mg/ml in dimethyl formamide |
pka | 15.12±0.46(Predicted) |
form | Pale yellow solid. |
Safety information for N-(2-PHENYLETHYL)-INDOMETHACIN AMIDE
Computed Descriptors for N-(2-PHENYLETHYL)-INDOMETHACIN AMIDE
New Products
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