1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. AZ 11645373

AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors,AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM.

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AZ 11645373 Chemical Structure

AZ 11645373 Chemical Structure

CAS No. : 227088-94-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors,AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM[1].

In Vitro

AZ11645373 produces a concentration-dependent inhibition of BzATP-mediated calcium transients, with complete inhibition observed at concentrations between 100 and 300 nM according to concentration-inhibition curves[1].
AZ11645373 inhibits ATP- or BzATP-evoked YO-PRO1 fluorescence in HEK cells stably expressing hP2X7R, but not in cells expressing rP2X7R, with an KB value not significantly different from those obtained in experiments measuring membrane currents or calcium mobilization[1].
AZ11645373 (0.01, 0.1, 1 μM; 30 min) has no significant effect on basal levels of IL-1β in culture medium of LPS-treated cells, but produces a concentration-dependent inhibition of ATP-mediated IL-1β release with a calculated KB value of 92 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

463.51

Formula

C24H21N3O5S

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1C(COC2=CC=C(C3=CC=CC([N+]([O-])=O)=C3)C=C2)CCC4=CC=NC=C4)SCC1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 17.5 mg/mL (37.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1575 mL 10.7873 mL 21.5745 mL
5 mM 0.4315 mL 2.1575 mL 4.3149 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1575 mL 10.7873 mL 21.5745 mL 53.9363 mL
5 mM 0.4315 mL 2.1575 mL 4.3149 mL 10.7873 mL
10 mM 0.2157 mL 1.0787 mL 2.1575 mL 5.3936 mL
15 mM 0.1438 mL 0.7192 mL 1.4383 mL 3.5958 mL
20 mM 0.1079 mL 0.5394 mL 1.0787 mL 2.6968 mL
25 mM 0.0863 mL 0.4315 mL 0.8630 mL 2.1575 mL
30 mM 0.0719 mL 0.3596 mL 0.7192 mL 1.7979 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AZ 11645373
Cat. No.:
HY-108670
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