192575-19-2

192575-19-2 structure

Name: PPADS tetrasodium salt
Chemical Name: Pyridoxal phosphate-6-azo(benzene-2,4-disulfonic acid) tetrasodium salt hydrate
CAS Number: 192575-19-2
Molecular Formula: C₁₄H₁₀N₃Na₄O₁₂PS₂
Molecular Weight: 599.305
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
Create Date: 2018-12-27 11:55:10
Modify Date: 2024-01-11 15:13:26
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].

Name	Pyridoxal phosphate-6-azo(benzene-2,4-disulfonic acid) tetrasodium salt hydrate
Synonyms	Tetrasodium 4-[(E)-{4-formyl-5-hydroxy-6-methyl-3-[(phosphonatooxy)methyl]pyridin-2-yl}diazenyl]benzene-1,3-disulfonate Tetrasodium 4-[(E)-{4-formyl-5-hydroxy-6-methyl-3-[(phosphonatooxy)methyl]-2-pyridinyl}diazenyl]-1,3-benzenedisulfonate PPADS (sodium salt) 1,3-Benzenedisulfonic acid, 4-[(E)-2-[4-formyl-5-hydroxy-6-methyl-3-[(phosphonooxy)methyl]-2-pyridinyl]diazenyl]-, sodium salt (1:4) MFCD11046026

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[1][2].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor Research Areas >> Neurological Disease
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 was 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: 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.
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.

Molecular Formula	C₁₄H₁₀N₃Na₄O₁₂PS₂
Molecular Weight	599.305
Exact Mass	598.903442
PSA	288.30000
LogP	3.77900
Storage condition	2-8°C

Safety Phrases	S22-S24/25

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