120210-48-2
Chemical Structure
Tenidap
Synonym(s): CP-66248
- CAS No.: 120210-48-2
- Formula:C14H9ClN2O3S
- Molecular Weight:320.75
IUPAC Name: (Z)-5-chloro-3-(hydroxy(thiophen-2-yl)methylene)-2-oxoindoline-1-carboxamide
InChIKey: LXIKEPCNDFVJKC-QXMHVHEDSA-N
SMILES: O/C(C1=CC=CS1)=C2C3=C(C=CC(Cl)=C3)N(C(N)=O)C/2=O
Biological Activity: Tenidap (CP-66248) is an orally active dual inhibitor of 5-LOX and COX with anti-inflammatory and immunomodulatory properties. Tenidap downregulates the expression of IL-1 receptors in chondrocytes, reduces the release of pro-inflammatory cytokines such as IL-1, IL-6 and TNF-α, and inhibits MMP production and cartilage degradation. Tenidap also blocks bone resorption and leukocyte adhesion to vascular endothelium, interferes with ion and pH changes associated with mouse sperm capacitation, and selectively enhances the activity of hKir2.3 channels (EC50=1.3 μM). Tenidap is applicable to research related to rheumatoid arthritis[1][2][3][4].
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Tenidap | 99.93% | Tenidap (CP-66248) is an orally active dual inhibitor of 5-LOX and COX with anti-inflammatory and immunomodulatory properties. Tenidap downregulates the expression of IL-1 receptors in chondrocytes, reduces the release of pro-inflammatory cytokines such as IL-1, IL-6 and TNF-α, and inhibits MMP production and cartilage degradation. Tenidap also blocks bone resorption and leukocyte adhesion to vascular endothelium, interferes with ion and pH changes associated with mouse sperm capacitation, and selectively enhances the activity of hKir2.3 channels (EC50=1.3 μM). Tenidap is applicable to research related to rheumatoid arthritis. | ||||||||||||||||||||
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Tenidap (Standard) | ≥98% | Tenidap (Standard) is the analytical standard of Tenidap. This product is intended for research and analytical applications. Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor. | ||||||||||||||||||||
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Tenidap-d3 | Tenidap-d3 is the deuterium labeled Tenidap. Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor. | |||||||||||||||||||||
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- [1]. Blackburn Jr W D, et al. Tenidap in rheumatoid arthritis a 24‐week double‐blind comparison with hydroxychloroquine‐plus‐piroxicam, and piroxicam alone[J]. Arthritis & Rheumatism, 1995, 38(10): 1447-1456.
- [2]. Breedveld F, et al. Tenidap: a novel cytokine-modulating antirheumatic drug for the treatment of rheumatoid arthritis. Scand J Rheumatol Suppl. 1994;100:31-44. [Content Brief]
- [3]. Chávez JC, et al. Participation of the Cl-/HCO(3)- exchangers SLC26A3 and SLC26A6, the Cl- channel CFTR, and the regulatory factor SLC9A3R1 in mouse sperm capacitation. Biol Reprod. 2012;86(1):1-14. Published 2012 Jan 19. [Content Brief]
- [4]. Liu Y, et al. Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K+ channel hKir2.3. Eur J Pharmacol. 2002;435(2-3):153-160. [Content Brief]
Keywords
