[CAS NO. 192575-19-2] PPADS tetrasodium
PRODUCTS SPECIFICATIONS [192575-19-2]
DESCRIPTION [192575-19-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 599.30 |
| Molecular Formula | C14H10N3Na4O12PS2 |
| SMILES | O=S(C1=CC=C(/N=N/C2=NC(C)=C(O)C(C=O)=C2COP(O[Na])(O[Na])=O)C(S(=O)(O[Na])=O)=C1)(O[Na])=O |
1 Publications Citing Use of MCE
Summary
PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC 50 s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like ( IC 50 ~0.9 mM) and recombinant P2Y4 ( IC 50 ~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca 2+ exchanger in guinea pig airway smooth muscle [1] [2] .
In Vitro
PPADS tetrasodiuma (1-30 μM; 10-50 minutes) inhibits Na+/Ca2+ exchanger reverse mode (NCXREV) in a time- and concentration dependent manner
[2]
.
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 IC
50
of ~1-3 and ~30 μM for the hP2X4R
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PPADS tetrasodiuma (15-60 mg/100g body weight (BW); i.p.; every 12 hours for 8 days) inhibits glomerular mesangial cells (MC) proliferation without altering proliferation of non-MC in vivo in mesangial proliferative glomerulonephritis [4] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague-Dawley ratsweighing 160 to 200 g (anti-Thy1 disease mode) [4] |
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 83.43 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6686 mL | 8.3431 mL | 16.6861 mL |
| 5 mM | 0.3337 mL | 1.6686 mL | 3.3372 mL |
| 10 mM | 0.1669 mL | 0.8343 mL | 1.6686 mL |
References
- [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.
- [2] Huo H, et al. Mapping the binding site of the P2X receptor antagonist PPADS reveals the importance of orthosteric site charge and the cysteine-rich head region. J Biol Chem. 2018 Aug 17;293(33):12820-12831.
- [3] Einfluss von ATP und seinen Derivaten auf die Aktivierung von Monozyten.
- [4] Rost S, et al. P2 receptor antagonist PPADS inhibits mesangial cell proliferation in experimental mesangialproliferative glomerulonephritis. Kidney Int. 2002 Nov;62(5):1659-71.