U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Status:
Designated
Source:
FDA ORPHAN DRUG:736720
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



ML355 is a potent and selective inhibitors of 12-Lipoxygenase(12-LOX) with IC50 of 0.34 uM. It has excellent selectivity over related lipoxygenases and cyclooxygenases. ML355 has favorable absorption, distribution, metabolism, and excretion (ADME) properties, inhibits PAR-4 induced aggregation and calcium mobilization in human platelets, and reduces 12-HETE in mouse/human beta cells suggesting its potential utility in animal models for antiplatelet therapy and diabetes.
1-Phenyl-3-pyrazolidinone (phenidone) is a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX). Phenidone inhibits both the LO (lipoxygenase) and Cox (cyclooxygenase) pathways, the synthesis of Fos-related antigen protein, and is described as an anti-inflammatory and anti-oxidant compound. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone was also the best in suppressing LPS induced neurotoxicity, where the more potent neuroprotection by phenidone may be attributable to the synergistic effects of dual COX and LOX inhibition. Therefore, dual inhibitors of COX and LOX, such as phenidone, represent valuable candidates for the development of novel drugs for inflammation-related neurodegenerative disorders including PD.
Status:
Possibly Marketed Outside US
Source:
ZUBRIN by Ortho-McNeil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tepoxalin is a nonsteroidal anti-inflammatory drug approved for veterinary use in the United States and many other countries. Marketed under the brand name Zubrin, Tepoxalin is indicated for the control of pain and inflammation associated with osteoarthritis in dogs. Tepoxalin has an unique property as an NSAIDs that suppresses both cyclooxygenase and lipoxygenase.