PPADS tetrasodium

CAS No. 192575-19-2

PPADS tetrasodium( —— )

Catalog No. M33471 CAS No. 192575-19-2

PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na/Ca2? exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate/NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    PPADS tetrasodium
  • Note
    Research use only, not for human use.
  • Brief Description
    PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na/Ca2? exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate/NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.
  • Description
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca2+ exchanger in guinea pig airway smooth muscle.
  • In Vitro
    PPADS tetrasodiuma (1-30 μM; 10-50 minutes) inhibits Na+/Ca2+ exchanger reverse mode (NCXREV) in a time- and concentration dependent manner.PPADS tetrasodiuma is effective at other native and recombinant P2XRs. At human P2XRs sensitivity to PPADS tetrasodiuma depended on the subtype and is highest at the hP2X1, -2, -3, -5, and -7Rs with an IC50 of ~1-3 and ~30 μM for the hP2X4R.
  • In Vivo
    PPADS tetrasodiuma (15-60 mg/100g body weight (BW); i.p.; every 12 hoursfor 8 days) inhibits glomerular mesangial cells (MC) proliferation without altering proliferation of non-MC in vivo in mesangial proliferative glomerulonephritis.Animal Model:Male Sprague-Dawley ratsweighing 160 to 200 g (anti-Thy1 disease mode)Dosage:15 mg/100g BW, 30 mg/100g BW, 60 mg/100g BW Administration:i.p.; every 12 hours for 8 days (the first PPADS injection was administered 60 minutes after disease induction, and the loading dose always contained double the amount of PPADS compared to the following injections.)Result:Specifically and dose-dependently reduced early (day 3) glomerular mesangial cell proliferation without altering proliferation of non-MC.
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    P2X Receptor
  • Recptor
    P2X Receptor | Na+/Ca2+ Exchanger
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    192575-19-2
  • Formula Weight
    599.3
  • Molecular Formula
    C14H10N3Na4O12PS2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?H2O : 50 mg/mL (83.43 mM; Ultrasonic)
  • SMILES
    O=CC1=C(C(C)=NC(N=NC2=CC=C(S(=O)([O-])=O)C=C2S(=O)([O-])=O)=C1COP([O-])([O-])=O)O.[Na+].[Na+].[Na+].[Na+]
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Flores-Soto E, et al. PPADS, a P2X receptor antagonist, as a novel inhibitor of the reverse mode of the Na?/Ca2? exchanger in guinea pig airway smooth muscle. Eur J Pharmacol. 2012 Jan 15;674(2-3):439-44.?
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