Every lot is tried & tested in a relevant biological assay.
- Caseley, E.A. et al. (2016) Biochem. Pharmacol. 116, 130.
- Alomone Labs ZINC58368839 inhibits human P2X7 receptors expressed in HEK-293 cells.Dose response curve of hP2X7 inhibition by ZINC58368839 (#Z-135). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of ZINC58368839, and stimulated with 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 13 µM.
ZINC58368839 inhibits P2X7 receptors by binding to the ATP-binding pocket of the receptor and demonstrates strong specificity towards human P2X7R over human P2X4R and rat P2X3R1. It inhibits BzATP-induced Ca2+ responses in HEK–hP2X7 cells with IC50 value of 4.8 µM1.
P2X receptors are cationic trimeric channel complexes that function as ATP-gated Ca2+-permeable channels. They are considered to be an attractive therapeutic target. This family includes seven receptor subtypes: P2X1–P2X7. P2X7 receptors participate in a variety of cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. P2X7 receptors are ubiquitously expressed, and particularly in cells of haematopoietic origin1,2.
ZINC58368839 (#Z-135) is a highly pure, synthetic, and biologically active compound.
- Anti-P2X7 Receptor Antibody (#APR-004)
- Anti-P2X7 Receptor-ATTO Fluor-550 Antibody (#APR-004-AO)
- Anti-P2X7 Receptor (extracellular) Antibody (#APR-008)
- Anti-P2X7 Receptor (extracellular)-ATTO Fluor-488 Antibody (#APR-008-AG)
- Anti-P2X7 Receptor (extracellular)-FITC Antibody (#APR-008-F)
- Anti-P2X7 Receptor (extracellular)-ATTO Fluor-633 Antibody (#APR-008-FR)
- HMA (#H-130)
- Chelerythrine chloride (#C-400)
- AZ11645373 (#A-395)
- AZ 10606120 dihydrochloride (#A-405)
- AACBA hydrochloride (#A-410)
- A-804598 (#A-415)
- A-740003 (#A-420)
- AZD-9056 hydrochloride (#A-425)
- A-839977 (#A-470)
- ZINC9315614 (#Z-145)
- JNJ-54166060 (#J-125)
- GW 791343 hydrochloride (#G-115)
- JNJ-47965567 (#J-115)
- KN-62 (#K-120)
- CAY10593 (VU0155069) (#C-385)
- Garcinolic acid (#G-155)
- BzATP triethylammonium salt (#A-385)