Fig. 1 · Structure

Documents & Downloads

A 740003

Cat. No. A11316 CAS 861393-28-4

P2X7 receptor antagonist

A 740003 is a novel competitive antagonist of P2X7 receptors (IC50 values = 40 nM for human and 18 nM for rat).

In Stock

Free Aliquoting for Your Order

Tell us your preferred amount per vial. We’ll confirm the options.

Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
HEK293 IC50 0.75 μM Antagonist activity at human P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 5 mins followed by ATP induction and measured after 25 mins by fluorescence assay [PMID: 30528164]
Peritoneal macrophage IC50 0.723 μM Antiinflammatory activity in LPS/IFNgamma-differentiated Swiss Webster mouse peritoneal macrophages assessed as inhibition of ATP-induced IL-1beta release preincubated for 15 mins followed by ATP/LPS challenge measured after 30 mins by sandwich ELISA [PMID: 29133043]
Peritoneal macrophage CC50 325.4 μM Cytotoxicity against Swiss Webster mouse peritoneal macrophages by LDH release assay [PMID: 29133043]
THP-1 IC50 0.689 μM Antiinflammatory activity in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of ATP-induced IL-1beta release after 30 mins by ELISA [PMID: 29133043]
THP-1 IC50 156 nM Antagonist activity at human recombinant P2X7 receptor expressed in human THP1 cells assessed as inhibition of BzATP-induced IL1-beta release by enzyme-linked immunosorbent assay [PMID: 19540765]

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 861393-28-4
Applications P2X7 receptor antagonist
Formula C26H30N6O3
Molecular Weight 474.6
SMILES
CC(C)(C)C(NC(=O)CC1=CC(=C(C=C1)OC)OC)/N=C(/NC#N)\NC2=CC=CC3=C2C=CC=N3

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 85 mg/mL (179.11 mM)
Water Insoluble
Ethanol 1 mg/mL

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Added to your cart

View Cart Checkout
Loading...