A hybrid molecule of an H2S donor and the NSAID diclofenac that does not cause gastric damage or promote leukocyte adherence to vascular endothelium; exhibits efficacy at doses of 10-50 µmole/kg in rat

ATB-337 – 10 mg

Brand:
Cayman
CAS:
912758-00-0
Storage:
-20
UN-No:
Non-Hazardous - /

Hydrogen sulfide (H2S) is a naturally occurring gasotransmitter with vasodilator and inflammatory modulating activity.{15636,15971} Non-steroidal anti-inflammatory drugs (NSAIDs), such as indomethacin, diclofenac, and ibuprofen, are some of the most commonly used anti-inflammatory drugs available but exhibit significant side effects, particularly gastric damage, when used chronically. ATB-337 is a hybrid molecule of an H2S donor and the NSAID diclofenac.{16442} In rats, diclofenac at 10-50 µmol/kg caused significant gastrointestinal damage, whereas no damage was observed with ATB-337 treatment at the same dose. ATB-337 at 50 µmol/kg does not promote leukocyte adherence to vascular endothelium, an effect observed with diclofenac treatment alone. COX-1 and COX-2 were inhibited with similar efficacy by diclofenac and ABT-337. An increase in expression of the pro-inflammatory mediator TNF-α, as well as, the adhesion molecules ICAM-1 and LFA-1 were not observed in rats treated with 50 µmol/kg ABT-337, effects seen with equimolar doses of diclofenac. These results indicate that H2S-releasing derivatives of NSAIDs may prove to be more effective anti-inflammatory agents than traditional NSAIDs alone.  

 

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Description

A hybrid molecule of an H2S donor and the NSAID diclofenac that does not cause gastric damage or promote leukocyte adherence to vascular endothelium; exhibits efficacy at doses of 10-50 µmole/kg in rat

Formal name: 2-[(2,6-dichlorophenyl)amino]-benzeneacetic acid, 4-(3-thioxo-3H-1,2-dithiol-5-yl)phenyl ester

Synonyms:  ACS 15|S-Diclofenac

Molecular weight: 504.5

CAS: 912758-00-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ox Stress Reagents|Hydrogen Sulfide Donors||Product Type|Biochemicals|Small Molecule Inhibitors|Cyclooxygenases||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Oxidative Stress & Reactive Species|Reactive Sulfur|H2S

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