A competitive antagonist of capsaicin activation of the TRPV1 (IC50s = 24.5 and 85.6 nM for human and rat

AMG 9810 – 50 mg

Brand:
Cayman
CAS:
545395-94-6
Storage:
-20
UN-No:
Non-Hazardous - /

AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively).{23388} Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine.{23388} In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.{23388}  

 

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Description

A competitive antagonist of capsaicin activation of the TRPV1 (IC50s = 24.5 and 85.6 nM for human and rat, respectively); reverses thermal and mechanical hyperalgesia in a rat model of inflammatory pain

Formal name: (2E)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide

Synonyms: 

Molecular weight: 337.4

CAS: 545395-94-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Immunology & Inflammation||Research Area|Neuroscience|Pain Research

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