Delving into the Latest Updates on WY 48989 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

IL-1α

Mechanism

IL-1α inhibitors(Interleukin-1 alpha inhibitors)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Rheumatoid Arthritis

Originator Organization

Wyeth AB

Active Organization-

Inactive Organization

Wyeth AB

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

Structure

Molecular FormulaC25H18ClN5

InChIKeyGYVYUQVVKBZPRY-UHFFFAOYSA-N

CAS Registry136917-40-3

The effects of potential anti-osteoarthritic compounds both on the direct inhibition of collagenase and neutral protease activities and on IL-1 induced release of neutral proteases from rabbit articular chondrocytes were investigated. WY-46,135 ((+)-N-[[[(5-chloro-2-benzothiazolyl)thio]phenyl]acetyl]-L- cysteine) directly inhibited collagenase activity (IC50 = 15.4 microM). This inhibition was reversible upon dialysis. WY-46,135 also directly inhibited neutral protease activity (IC50 = 16.8 microM) but did not significantly block bacterial collagenase activity at a concentration of 80 microM. In contrast, WY-48,989 (4-[[2-(7-chloro-2-phenyl-2H-pyrazolo[4,3-c]quinolin-4- yl)ethyl]amino]benzonitrile) did not directly inhibit either collagenase (10 microM) or neutral protease (100 microM) activity. Both WY-48,989 and WY-46,135 inhibited IL-1 stimulated release of neutral proteases (IC50 = 3 microM). The activities of these compounds represents two potential approaches for the treatment of osteoarthritis. WY-46,135 combines direct metalloprotease inhibitory activity with the inhibition of IL-1 stimulated neutral protease release from articular chondrocytes while WY-48,989 selectively inhibits the IL-1 induced release of metalloproteases.

100 Deals associated with WY 48989

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