A TRPV1 antagonist (IC50 = 0.9 nM); inhibits mechanical and thermal allodynia in a rat model of burn injury at 165 µg

AMG 517 – 50 mg

Brand:
Cayman
CAS:
659730-32-2
Storage:
-20
UN-No:
Non-Hazardous - /

AMG 517 is an antagonist of transient receptor potential vanilloid 1 (TRPV1; IC50 = 0.9 nM).{45105} It inhibits mechanical and thermal allodynia in a rat model of burn injury when administered intrathecally at a dose of 165 µg.{35412} AMG 517 (150 and 300 µg/kg) also reverses increases in the level of calcitonin gene-related peptide (CGRP) and increases expression of GFAP and GAP-43 in the dorsal horn of the spinal cord, as well as enhances axonal regeneration in a rat model of sciatic nerve transection injury.{45106}  

 

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Description

A TRPV1 antagonist (IC50 = 0.9 nM); inhibits mechanical and thermal allodynia in a rat model of burn injury at 165 µg, intrathecally; reverses increases in the level of CGRP and increases expression of GFAP and GAP-43 in the dorsal horn of the spinal cord, as well as enhances axonal regeneration in a rat model of sciatic nerve transection injury

Formal name: N-[4-[[6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]-acetamide

Synonyms: 

Molecular weight: 430.4

CAS: 659730-32-2

Purity: ≥98%

Formulation: A crystalline solid

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

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