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74252-25-8

74252-25-8 structure
74252-25-8 structure
  • Name: Indomethacin sodium hydrate
  • Chemical Name: sodium,2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetate,trihydrate
  • CAS Number: 74252-25-8
  • Molecular Formula: C19H21ClNNaO7
  • Molecular Weight: 357.788
  • Catalog: Signaling Pathways Autophagy Autophagy
  • Create Date: 2018-06-08 17:30:53
  • Modify Date: 2024-01-02 22:24:27
  • Indomethacin sodium hydrate (Indometacin sodium hydrate) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin sodium hydrate disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].

Name sodium,2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetate,trihydrate
Synonyms Catlep
Indomethacinum
1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-
Indomethacin sodium (USP)
1H-Indole-3-acetic acid,1-(4-chlorobenzoyl)-5-methoxy-2-methyl-,sodium salt,trihydrate
Indomethacine
{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}acetic acid
Durametacin
UNII-0IMX38M2GG
[1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
Dolcidium
Indomethacin sodium trihydrate
Chrono-indocid
Sodium 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetate,trihydrate
Indometacin sodium (JAN)
indometacin
Na salt,tri-H2O
Indomethacin
Indocin I.V. (TN)
Chibro-amuno
Bonidon
Description Indomethacin sodium hydrate (Indometacin sodium hydrate) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin sodium hydrate disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
Related Catalog
In Vitro Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin inhibits lipopolysaccharide (LPS)-induced PGE2 production (COX-2) in a human whole blood assay with a potency (IC50=0.68±0.17 μM), and suppresses coagulation-induced TXB2 production (COX-1) (IC50=0.19±0.02 μM). Indomethacin blocks COX-1 with an IC50 of 20±1 nM in U937 cell microsomes at a low arachidonic acid concentration (0.1 μM)[1].
In Vivo Indomethacin dose-dependently inhibits both the carrageenan-induced rat paw oedema (ED50, 2.0 mg/kg), hyperalgesia (ED50, 1.5 mg/kg), and is also effective at reversing LPS-induced pyrexia in rats (ED50, 1.1 mg/kg)[1]. Indomethacin (2.5 mg/kg, i.p) decreases the number of NeuN+ cells in the animals at 8 days after ET-1 injection. Indomethacin also reduces microglia/macrophage activation at 14 days. Indomethacin significantly increases the number of SVZ DCX+ cells/field at 14 days post stroke[3]. Indomethacin (22.9 mg/kg, p.o.) produces 8 to 10 linear mucosal lesions extended from the fundic to pyloric area of stomach wall[4].
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]. Jorge Vallecillo-Hernández, et al. Indomethacin Disrupts Autophagic Flux by Inducing Lysosomal Dysfunction in Gastric Cancer Cells and Increases Their Sensitivity to Cytotoxic Drugs. Sci Rep. 2018 Feb 26;8(1):3593.

[3]. Lopes RS, et al. Indomethacin treatment reduces microglia activation and increases numbers of neuroblasts in the subventricular zone and ischaemic striatum after focal ischaemia. J Biosci. 2016 Sep;41(3):381-94.

[4]. Afroz S, et al. Concentrated phosphatidic acid in cereal brans as potential protective agents against indomethacin-induced stomach ulcer. J Agric Food Chem. 2016 Aug 26.

Density 1.3±0.1 g/cm3
Boiling Point 499.4±45.0 °C at 760 mmHg
Melting Point 162ºC
Molecular Formula C19H21ClNNaO7
Molecular Weight 357.788
Flash Point 255.8±28.7 °C
Exact Mass 357.076782
PSA 99.05000
LogP 3.11
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.619
Storage condition -20℃