PPADS tetrasodium_product_DataBase

Bioactivity	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[1][2].
Invitro	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 IC50 of ~1-3 and ~30 μM for the hP2X4R[3].
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]. Animal Model:
Name	PPADS tetrasodium
CAS	192575-19-2
Formula	C14H10N3Na4O12PS2
Molar Mass	599.30
Appearance	Solid
Transport	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)
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. [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.

PeptideDB

PPADS tetrasodium

CAS: 192575-19-2 F: C14H10N3Na4O12PS2 W: 599.30