5.08317
A740003
别名:
A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
InChI
1S/C26H30N6O3/c1-26(2,3)24(31-23(33)15-17-11-12-21(34-4)22(14-17)35-5)32-25(29-16-27)30-20-10-6-9-19-18(20)8-7-13-28-19/h6-14,24H,15H2,1-5H3,(H,31,33)(H2,29,30,32)
InChI key
PUHSRMSFDASMAE-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
potency
18 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 30 mg/mL
storage temp.
2-8°C
Quality Level
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Preparation Note
Slight warming is required for complete solubilization.
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Biochem/physiol Actions
Primary Target
P2X7
P2X7
Disclaimer
Toxicity: Standard Handling (A)
General description
A highly potent, selective, competitive antagonist of P2X7 purinegic receptor (IC50 = 18 nM and 40 nM, respectively as measured by Bz-ATP-stimulated Ca2+ flux). Does not affect other P2 receptors even at 10 µM concentrations. Blocks agonist-evoked IL-1b release (IC50 = 156 nM) and pore formation (IC50 = 92 nM) in differentiated human THP-1 cells. Also shown to reduce carrageenan and Freund′s adjuvant -induced thermal hyperalgesia (ED50 = 38-54 mg/kg, i.p) and neuropathic pain induced by chronic constriction injury (CIC) of the sciatic nerve.
Other Notes
Honore, P., et al. 2006. J. Pharmacol. Exp. Ther.319, 1376.
Packaging
Packaged under inert gas
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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