A P2X7 receptor antagonist
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NSC 102533

Item No. 42435

Technical Information
Formal Name
2-hydroxy-3-phenyl-1,4-naphthalenedione
CAS Number
1150-59-0
Synonyms
  • AN-04
Molecular Formula
C16H10O3
Formula Weight
Purity
≥95%
A solid
DMSO: Sparingly Soluble: 1-10 mg/mLEthanol: Slightly Soluble: 0.1-1 mg/mL
SMILES
O=C1C(O)=C(C(C2=C1C=CC=C2)=O)C3=CC=CC=C3
InChi Code
InChI=1S/C16H10O3/c17-14-11-8-4-5-9-12(11)15(18)16(19)13(14)10-6-2-1-3-7-10/h1-9,19H
InChi Key
KUKDVSFMDRAXML-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NSC 102533 is an antagonist of the purinergic P2X7 receptor.1 It inhibits ATP-induced dye uptake in HEK293 cells expressing human purinergic P2X7 receptors (IC50 = 22.4 nM). NSC 102533 also inhibits common lancehead (B. atrox) venom proteolysis in a concentration-dependent manner.2 It inhibits ATP-induced IL-1ß secretion in human THP-1 monocytes and primary mouse peritoneal macrophages (IC50s = 9.8 and 11.2 nM, respectively).1 Intradermal administration of NSC 102533 (3 mg/kg) inhibits common lancehead (B. atrox) and jararaca (B. jararaca) venom-induced skin hemorrhage in mice.2 It inhibits carrageenan-induced paw edema in mice when administered at doses ranging from 0.01 to 1 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Faria, R.X., Oliveira, F.H., Salles, J.P., et al. 1,4-Naphthoquinones potently inhibiting P2X7 receptor activity. Eur. J. Med. Chem. 143, 1361-1372 (2018).

    2. Strauch, M.A., Tomaz, M.A., Monteiro-Machado, M., et al. Lapachol and synthetic derivatives: In vitro and in vivo activities against Bothrops snake venoms. PLoS One 14(1), (2019).