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5.08317

A740003

Synonym(s):

A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003

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About This Item

Empirical Formula (Hill Notation):
C26H30N6O3
CAS Number:
861393-28-4
Molecular Weight:
474.55
UNSPSC Code:
12352200
MDL number:
MFCD09970333
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, protect from light
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assay

≥98% (HPLC)

Quality Level

100

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

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

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.

Biochem/physiol Actions

Primary Target
P2X7

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Slight warming is required for complete solubilization.

Other Notes

Honore, P., et al. 2006. J. Pharmacol. Exp. Ther.319, 1376.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Global Trade Item Number

SKUGTIN
508317000104055977261851