INDOMETHACIN SODIUM

Names

[ Name ]:
INDOMETHACIN SODIUM

[Synonym ]:
Sodium [1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetate
EINECS 231-670-4
INDOMETHACIN SODIUM
Na salt
1H-Indole-3-acetic acid,1-(4-chlorobenzoyl)-5-methoxy-2-methyl-,sodium salt
Sodium indomethacin
Sodium 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetate
1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-, sodium salt (1:1)
Osmosin

Biological Activity

[Description]:

Indomethacin (Indometacin) sodium is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin sodium has anticancer activity and anti-infective activity. Indomethacin sodium can be used for cancer, inflammation and viral infection research.[1][2][3].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> Influenza Virus

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Immunology/Inflammation >> COX

[Target]

COX-1:18 nM (IC50)

COX-2:26 nM (IC50)

[In Vitro]

Indomethacin (Indometacin) sodium (0-150 μM; 24 hours; 3LL-D122 cells) has anticancer activity in vitro[2]. Indomethacin (Indometacin) sodium (0-1000 μM) protects the host cells from damage caused by the virus through activates PKR, resulting in elF2α phosphorylation, and in turn shutting of translation of viral protein and inhibiting replication of the virus (IC50=2μM)[3]. Cell Viability Assay[2] Cell Line: 3LL-D122 cells (highly metastatic variant of mouse LLcarcinoma cells) Concentration: 0, 20, 50, 100 and 150μM Incubation Time: 24 hours Result: Inhibited cell viability at 20 mM, with 50% inhibition at 60 nM. Cell Cycle Analysis[2] Cell Line: 3LL-D122 cells (highly metastatic variant of mouse LLcarcinoma cells) Concentration: 0, 30 and 80μM Incubation Time: 24 hours Result: Decreased in the percentage of cells at the G2/M phase and increased in the percentage of cells at G1 phase.

[In Vivo]

Indomethacin (Indometacin) sodium (0.01-10 mg/kg; p.o.; for 3 hours; male Sprague-Dawley rats) induces paw oedema and hyperalgesmeasurement dose-dependently reversed carrageenan-induced hyperalgesia[1]. Indomethacin (Indometacin) sodium (10 mg/mL; p.o.; daily, for 29 days; male C57BL/6J mice) inhibits tumor growth in vivo[2]. Animal Model: Male Sprague-Dawley rats[1] Dosage: 0.01-10 mg/kg Administration: Oral administration; for 3 hours Result: Inhibited the carrageenan-induced rat paw oedema (ED50=2.0 mg/kg) and hyperalgesia (ED50=1.5 mg/kg) in a dose-dependent manner. Animal Model: Male C57BL/6J mice[2] Dosage: 10 mg/mL Administration: Oral administration; daily, for 29 days Result: Delayed the onset of tumor growth and the initial growth rate of the footpad tumors.

[References]

[1]. Riendeau D, et, al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.

[2]. Amici C, et, al. Inhibition of viral protein translation by indomethacin in vesicular stomatitis virus infection: role of eIF2α kinase PKR. Cell Microbiol. 2015 Sep;17(9):1391-404.

[3]. Eli Y, et, al. Comparative effects of indomethacin on cell proliferation and cell cycle progression in tumor cells grown in vitro and in vivo. Biochem Pharmacol. 2001 Mar 1;61(5):565-71.

Chemical & Physical Properties

[ Melting Point ]:
162ºC

[ Molecular Formula ]:
C₁₉H₁₅ClNNaO₄

[ Molecular Weight ]:
379.770

[ Exact Mass ]:
379.058716

[ PSA ]:
71.36000

[ LogP ]:
2.59260

Safety Information

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%