1268882-21-8

Basic information

• Product Name: (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid ((S)-2-hydroxy-1-phenyl-ethyl)-amide
• CAS NO: 1268882-21-8
• Molecular Weight: 377.403
• Mol File: 1268882-21-8.mol
• Article Data: 2

Chemical Properties

• CAS DataBase Reference: (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid ((S)-2-hydroxy-1-phenyl-ethyl)-amide(CAS DataBase Reference)
• NIST Chemistry Reference: (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid ((S)-2-hydroxy-1-phenyl-ethyl)-amide(1268882-21-8)
• EPA Substance Registry System: (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid ((S)-2-hydroxy-1-phenyl-ethyl)-amide(1268882-21-8)

Safety Data

• Hazardous Substances Data: 1268882-21-8(Hazardous Substances Data)

Upstream product

• 822-58-2 (1R,2R,5S)-bicyclo[3.1.0]hexan-2-ol 
• 137688-21-2 (-)-(S)-2-(but-3-enyl)oxirane 
• 1268883-00-6 3-((4aS,5aS)-3-carboxy-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazol-1-yl)pyrazine 1-oxide 
• 20989-17-7 (2S)-2-phenylglycinol 
• 1268883-11-9 (1aS,5aS)-2-(pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid ethyl ester 
• 196488-92-3 (1S,5R)-bicyclo[3.1.0]hexan-2-one 

Relevant articles and documents

Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain

The discovery of a novel, selective and fully efficacious CB2 agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound 6 was efficacious in a rat model of osteoarthritis pain following oral administration and, in contrast to morphine, maintained its analgesic effect throughout a 5-day subchronic treatment paradigm. These data were consistent with our hypothesis that full agonist efficacy is required for efficient internalization and recycling of the CB2 receptor to avoid tachyphylaxis. Based on its overall favorable preclinical profile, 6 (APD371) was selected for further development for the treatment of pain.