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About This Item
Empirical Formula (Hill Notation):
C19H15F6N3O3S
CAS Number:
Molecular Weight:
479.40
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Brain-penetrant, orally active, potent and selective transient receptor potential cation channel TRPV1 antagonist with in vivo analgesia efficacy.
A-784168 is a brain-penetrant, orally active, potent and selective transient receptor potential (TRP) cation channel TRPV1 antagonist (IC50 = 25/14/33.7/35.1 nM against TRPV1 activation by 50 nM capsaicin/pH 5.5/3 µM NADA/10 µM anandamide in human TRPV1 tranfectants) with little activity or affinity toward other TRP channels and a panel of 74 neurotransmitter receptors. A-784168 reduces capsaicin-induced acute pain (ED50 = 10 µmol/kg p.o. 1h before capsaicin intraplantar injection) and CFA paw injection-induced chronic inflammatory thermal hyperalgesia (EC50 = 54 nmol) in rats in vivo.
A-784168 is a brain-penetrant, orally active, potent and selective transient receptor potential (TRP) cation channel TRPV1 antagonist (IC50 = 25/14/33.7/35.1 nM against TRPV1 activation by 50 nM capsaicin/pH 5.5/3 µM NADA/10 µM anandamide in human TRPV1 tranfectants) with little activity or affinity toward other TRP channels and a panel of 74 neurotransmitter receptors. A-784168 reduces capsaicin-induced acute pain (ED50 = 10 µmol/kg p.o. 1h before capsaicin intraplantar injection) and CFA paw injection-induced chronic inflammatory thermal hyperalgesia (EC50 = 54 nmol) in rats in vivo.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
Storage Class
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Characterization of nerve growth factor-induced mechanical and thermal hypersensitivity in rats
European Journal of Pain, 17(4), 469-479 (2013)
Role of TRPV1 and ASIC3 in formalin-induced secondary allodynia and hyperalgesia
Pharmacological Reports, 66(6), 964-971 (2014)
TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists
The Journal of Neuroscience, 26(37), 9385-9393 (2006)
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