142741-60-4
Chemical Structure
Tenidap-d3
Synonym(s): CP-66248-d3
- CAS No.: 142741-60-4
- Formula:C14H6D3ClN2O3S
- Molecular Weight:323.77
IUPAC Name: (Z)-5-chloro-3-(hydroxy(thiophen-2-yl-d3)methylene)-2-oxoindoline-1-carboxamide
InChIKey: LXIKEPCNDFVJKC-DVVZZJNRSA-N
SMILES: O/C(C1=C([2H])C([2H])=C([2H])S1)=C2C3=C(C=CC(Cl)=C3)N(C(N)=O)C/2=O
Biological Activity: 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[1][2]. Tenidap is also a specific SLC26A3 inhibitor[3].
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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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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 | 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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- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
- [2]. Kirchner T, et al. 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. 1997 Aug;282(2):1094-101. [Content Brief]
- [3]. Blackburn WD Jr, et al. Tenidap in rheumatoid arthritis. A 24-week double-blind comparison with hydroxychloroquine-plus-piroxicam, and piroxicam alone. Arthritis Rheum. 1995 Oct;38(10):1447-56. [Content Brief]
Keywords
