Product Data Sheet
NSC 102533
Catalog No. A22680
NSC 102533 is a potent antagonist of the purinergic P2X7 receptor, a ligand-gated ion channel involved in inflammation and immune regulation. It effectively inhibits ATP-induced dye uptake in HEK293 cells expressing human P2X7 receptors with an IC₅₀ of 22.4 nM. NSC 102533 also suppresses ATP-induced IL-1β secretion in human THP-1 monocytes and primary mouse peritoneal macrophages, with IC₅₀ values of 9.8 nM and 11.2 nM, respectively, demonstrating strong anti-inflammatory activity.
In addition to its immunomodulatory effects, NSC 102533 exhibits antivenom potential by inhibiting Bothrops atrox venom proteolysis in a concentration-dependent manner. In in vivo studies, intradermal administration of NSC 102533 (3 mg/kg) significantly reduces skin hemorrhage induced by B. atrox and B. jararaca venom and attenuates carrageenan-induced paw edema in mice at doses between 0.01 and 1 mg/kg. These properties highlight NSC 102533 as a valuable pharmacological tool for studying P2X7 receptor–mediated inflammatory responses and venom-induced pathology.
| Catalog Num | A22680 |
|---|---|
| M. Wt | 250.25 |
| Formula | C16H10O3 |
| Purity | >98% |
| Storage | at -20 °C 3 years (powder form); at -20 °C 6 months (Solution base) |
| CAS No. | 1150-59-0 |
| Synonyms | NSC102533,NSC-102533 |
| SMILES | C1=CC=C(C=C1)C2=C(C3=CC=CC=C3C(=O)C2=O)O |
| Description | NSC 102533 is a potent antagonist of the purinergic P2X7 receptor, a ligand-gated ion channel involved in inflammation and immune regulation. It effectively inhibits ATP-induced dye uptake in HEK293 cells expressing human P2X7 receptors with an IC₅₀ of 22.4 nM. NSC 102533 also suppresses ATP-induced IL-1β secretion in human THP-1 monocytes and primary mouse peritoneal macrophages, with IC₅₀ values of 9.8 nM and 11.2 nM, respectively, demonstrating strong anti-inflammatory activity. In addition to its immunomodulatory effects, NSC 102533 exhibits antivenom potential by inhibiting Bothrops atrox venom proteolysis in a concentration-dependent manner. In in vivo studies, intradermal administration of NSC 102533 (3 mg/kg) significantly reduces skin hemorrhage induced by B. atrox and B. jararaca venom and attenuates carrageenan-induced paw edema in mice at doses between 0.01 and 1 mg/kg. These properties highlight NSC 102533 as a valuable pharmacological tool for studying P2X7 receptor–mediated inflammatory responses and venom-induced pathology. |
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