Description: NSAID, cyclooxygenase (COX-1) inhibitor. Also opener of KIR2.3
Alternative Names: CP 66248
Chemical Name: (Z)-5-Chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indole-1-carboxamide
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
NSAID that preferentially inhibits COX-1 (IC50 values are < 0.03, 1.2 and > 30 μM for COX-1, COX-2 and 5-lipoxygenase respectively). Inhibits formation of pro-inflammatory arachidonic acid metabolites in isolated human peripheral polymorphonuclear leukocytes. Opener of inward rectifying hKir2.3 channel (EC50 = 402 nM).
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Technical Data
M. Wt
320.75
Formula
C14H9N2O3SCl
Storage
Store at +4°C
Purity
≥99% (HPLC)
CAS Number
120210-48-2
PubChem ID
54683953
InChI Key
LXIKEPCNDFVJKC-QXMHVHEDSA-N
Smiles
O=C1N(C(N)=O)C2=CC=C(Cl)C=C2/C1=C(O)C3=CC=CS3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
32.07
100
Preparing Stock Solutions
The following data is based on the product molecular weight 320.75. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
3.12 mL
15.59 mL
31.18 mL
5 mM
0.62 mL
3.12 mL
6.24 mL
10 mM
0.31 mL
1.56 mL
3.12 mL
50 mM
0.06 mL
0.31 mL
0.62 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Moilanenet al (1988) CP-66,248, a new anti-inflammatory agent, is a potent inhibitor of leukotriene B4 and prostanoid synthesis in human polymorphonuclear leucocytes in vitro. Eicosanoids 1 35 PMID: 2856170
Kirchneret al (1997) Evaluation of the antiinflammatory activity of a dual cyclooxygenase-2 selective/5-lipoxygenase inhibitor, RWJ 63556, in a canine model of inflammation. J.Pharmacol.Exp.Ther. 282 1094 PMID: 9262379
Liuet al (2002) Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K+ channel hKir2.3. Eur.J.Pharmacol. 435 153 PMID: 11821021