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Key Documents

5.05315

Sigma-Aldrich

A 438079

Synonym(s):

A 438079, 3-((5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl)methyl)pyridine hydrochloride, P2X7 Purinergic Receptor Antagonist, A 438079, A438079, A-438079

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About This Item

Empirical Formula (Hill Notation):
C13H9Cl2N5 · xHCl
CAS Number:
899507-36-9
Molecular Weight:
306.15 (free base basis)
UNSPSC Code:
12352200

Assay

≥99% (HPLC)

Quality Level

100

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mM

storage temp.

2-8°C

InChI

1S/C13H9Cl2N5.ClH/c14-11-5-1-4-10(12(11)15)13-17-18-19-20(13)8-9-3-2-6-16-7-9;/h1-7H,8H2;1H

InChI key

MBTJFFMIPPMRGR-UHFFFAOYSA-N

General description

A potent, competitive, and selective antagonist of P2X7 purinergic receptor (pIC50 = 6.5 nM and 6.9 nM for rat and human P2X7 receptor, respectively). Shown to reduce ATP-induced reactive oxygen species formation in MEL cells by about 87% (~10 µM) and blocks BzATP-stimulated changes in intracellular calcium concentrations (IC50 = 100 and 300 nM at rat and human P2X7 receptors, respectively.

Biochem/physiol Actions

Primary Target
P2X₇

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Donnelly-Roberts, et al., 2007, Br. J. Pharmacol.101, 571.

Wang B, et al., 2013, Purinergic Signal.9, 101.

Legal Information

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

Storage Class Code

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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D L Donnelly-Roberts et al.
British journal of pharmacology, 151(5), 571-579 (2007-05-02)
ATP-sensitive P2X(7) receptors are localized on cells of immunological origin including peripheral macrophages and glial cells in the CNS. Activation of P2X(7) receptors leads to rapid changes in intracellular calcium concentrations, release of the proinflammatory cytokine interleukin-1beta and following prolonged
Bin Wang et al.
Purinergic signalling, 9(1), 101-112 (2012-09-28)
The presence of P2X7 on erythroid cells is well established, but its physiological role remains unclear. The current study aimed to determine if P2X7 activation induces reactive oxygen species (ROS) formation in murine erythroleukaemia (MEL) cells, a commonly used erythroid

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