119784-94-0
Chemical Structure
Tenidap sodium
Synonym(s): CP-66248 sodium
- CAS No.: 119784-94-0
- Formula:C14H8ClN2NaO3S
- Molecular Weight:342.73
IUPAC Name: sodium (Z)-(1-carbamoyl-5-chloro-2-oxoindolin-3-ylidene)(thiophen-2-yl)methanolate
InChIKey: VCSAHSDZAKGXAT-AFEZEDKISA-M
SMILES: O=C1/C(C2=CC(Cl)=CC=C2N1C(N)=O)=C(C3=CC=CS3)\O[Na]
Biological Activity: Tenidap (CP-66248) sodium is an orally active cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitor. Tenidap sodium exerts anti-inflammatory and chondroprotective effects by downregulating IL-1 receptor expression, reducing the release of pro-inflammatory cytokines, and inhibiting metalloproteinase and acute-phase protein production, while also inhibiting SLC26A3-mediated chloride transport and the pH and membrane potential changes associated with sperm capacitation. Tenidap sodium attenuates carrageenan-induced paw edema and acetic acid-induced writhing, and induces gastric ulcers in a dose-dependent manner, and can be used for research on rheumatoid arthritis[1][2][3][4][5].
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Tenidap sodium | Tenidap (CP-66248) sodium is an orally active cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitor. Tenidap sodium exerts anti-inflammatory and chondroprotective effects by downregulating IL-1 receptor expression, reducing the release of pro-inflammatory cytokines, and inhibiting metalloproteinase and acute-phase protein production, while also inhibiting SLC26A3-mediated chloride transport and the pH and membrane potential changes associated with sperm capacitation. Tenidap sodium attenuates carrageenan-induced paw edema and acetic acid-induced writhing, and induces gastric ulcers in a dose-dependent manner, and can be used for research on rheumatoid arthritis. | |||||||||||||||||||||
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References
- [1]. Blackburn, et al. (1995), Tenidap in rheumatoid arthritis a 24-week double-blind comparison with hydroxychloroquine-plus-piroxicam, and piroxicam alone. Arthritis & Rheumatism, 38: 1447-1456.
- [2]. Breedveld F, et al. Tenidap: a novel cytokine-modulating antirheumatic drug for the treatment of rheumatoid arthritis. Scandinavian journal of rheumatology. Supplement. 1994;100:31-44. [Content Brief]
- [3]. Julio C, et al. Participation of the Cl−/HCO3− Exchangers SLC26A3 and SLC26A6, the Cl− Channel CFTR, and the Regulatory Factor SLC9A3R1 in Mouse Sperm Capacitation, Biology of Reproduction, Volume 86, Issue 1, 1 January 2012, 14, 1-14.
- [4]. Yi Liu, et al. Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K+ channel hKir2.3, European Journal of Pharmacology, Volume 435, Issues 2-3, 2002, Pages 153-160, ISSN 0014-2999.
- [5]. Lai Y, et al. Synthesis and biological evaluation of 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives as novel COX-1/2 and 5-LOX inhibitors. Bioorganic & medicinal chemistry letters. 2010 Dec 15;20(24):7349-53. [Content Brief]
