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Submit ReviewPPADS tetrasodium salt
Description: Non-selective P2 antagonist
Chemical Name: Pyridoxalphosphate-6-azophenyl-2',4'-disulfonic acid tetrasodium salt
Biological Activity for PPADS tetrasodium salt
PPADS tetrasodium salt is a non-selective P2 purinergic antagonist. Blocks recombinant P2X1, P2X2, P2X3, P2X5 (IC50 = 1 - 2.6 μM), native P2Y2-like (IC50 ~ 0.9 mM), and recombinant P2Y4 (IC50 ~ 15 mM) receptors. PPADS tetrasodium salt delays onset of calcium responses to mild hypoosmotic stress in cortical slices. PPADS tetrasodium salt blocks P2X7 and reduces clinical and histological graft-versus-host disease development in a humanised mouse model.
2'5'-isomer also available.
Technical Data for PPADS tetrasodium salt
| M. Wt | 599.3 |
| Formula | C14H10N3Na4O12PS2 |
| Storage | Desiccate at -20°C |
| CAS Number | 192575-19-2 |
| PubChem ID | 101086948 |
| InChI Key | KURWUCJJNVPCHT-UHFFFAOYSA-J |
| Smiles | [Na+].[Na+].[Na+].[Na+].CC1=C(O)C(C=O)=C(COP([O-])([O-])=O)C(\N=N\C2=C(C=C(C=C2)S([O-])(=O)=O)S([O-])(=O)=O)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PPADS tetrasodium salt
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 100 |
Preparing Stock Solutions for PPADS tetrasodium salt
The following data is based on the product molecular weight 599.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.67 mL | 8.34 mL | 16.69 mL |
| 5 mM | 0.33 mL | 1.67 mL | 3.34 mL |
| 10 mM | 0.17 mL | 0.83 mL | 1.67 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
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Product Datasheets for PPADS tetrasodium salt
References for PPADS tetrasodium salt
References are publications that support the biological activity of the product.
Ziganshin et al (1994) Selective antagonism by PPADS at P2x-purinoceptors in rabbit isolated blood vessels. Br.J.Pharmacol. 111 923 PMID: 8019770
Lambrecht et al (1992) PPADS, a novel functionally selective antagonist of P2 purinoceptor-mediated responses. Eur.J.Pharmacol. 217 217 PMID: 1330591
McLaren et al (1994) Investigation of the actions of PPADS, a novel P2x-purinoceptor antagonist, in the guinea-pig isolated vas deferens. Br.J.Pharmacol. 111 913 PMID: 8019769
Ralevic and Burnstock (1998) Receptors for purines and pyrimidines. Pharmacol.Rev. 50 413 PMID: 9755289
Thrane et al (2011) Critical role of aquaporin-4 (AQP4) in astrocytic Ca2+ signaling events elicited by cerebral edema. Proc.Natl.Acad.Sci.U S A 108 846 PMID: 21187412
Cuthbertson et al (2021) P2X7 receptor antagonism increases regulatory T cells and reduces clinical and histological graft-versus-host disease in a humanised mouse model. Clin.Sci. 135 495 PMID: 33463682
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Keywords: PPADS tetrasodium salt, PPADS tetrasodium salt supplier, P2, purinergic, antagonists, P2X, Receptors, Purinergic, P2Y, purinoceptors, antagonises, inhibitors, inhibits, 0625, Tocris Bioscience
26 Citations for PPADS tetrasodium salt
Citations are publications that use Tocris products. Selected citations for PPADS tetrasodium salt include:
Ievglevskyi et al (2012) Modulation of ATP-induced LTP by cannabinoid receptors in rat hippocampus. Purinergic Signal 8 705 PMID: 22453905
Cheung et al (2015) Pharmacological and molecular characterization of functional P2 receptors in rat embryonic cardiomyocytes. J Mol Neurosci 11 127 PMID: 25510459
Zhang et al (2016) Signaling mechanism for modulation by ATP of glycine receptors on rat retinal ganglion cells. Sci Rep 6 28938 PMID: 27357477
Yamashita et al (2016) Duloxetine inhibits microglial P2X4 receptor function and alleviates neuropathic pain after peripheral nerve injury PLoS One 11 e0165189 PMID: 27768754
Gómez-Gonzalo et al (2010) An excitatory loop with astrocytes contributes to drive neurons to seizure threshold. PLoS Biol 8 e1000352 PMID: 20405049
Rodríguez-Zayas et al (2012) Blockade of P2 nucleotide receptors after spinal cord injury reduced the gliotic response and spared tissue. Neuropsychopharmacology 46 167 PMID: 21647706
Pozner et al (2015) Intracellular calcium dynamics in cortical microglia responding to focal laser injury in the PC::G5-tdT reporter mouse. Front Mol Neurosci 8 12 PMID: 26005403
Fonseca et al (2015) Diadenosine tetraphosphate contributes to CB-induced tear secretion. Purinergic Signal 11 87 PMID: 25398705
Kouzaki et al (2011) The danger signal, extracellular ATP, is a sensor for an airborne allergen and triggers IL-33 release and innate Th2-type responses. J Immunol 186 4375 PMID: 21357533
Thrane et al (2011) Critical role of aquaporin-4 (AQP4) in astrocytic Ca2+ signaling events elicited by cerebral edema. Proc Natl Acad Sci U S A 108 846 PMID: 21187412
Miguel Cruz & Beall (2020) Extracellular ATP Increases Glucose Metabolism in Skeletal Muscle Cells in a P2 Receptor Dependent Manner but Does Not Contribute to Palmitate-Induced Insulin Resistance. Front Physiol 11 567378 PMID: 33101053
Bulavina et al (2013) NTPDase1 activity attenuates microglial phagocytosis. Purinergic Signal 9 199 PMID: 23208703
Cuthbertson et al (2021) P2X7 receptor antagonism increases regulatory T cells and reduces clinical and histological graft-versus-host disease in a humanised mouse model. Clin.Sci. 135 495 PMID: 33463682
McEwan et al (2021) Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation Life Sci 283 119850 PMID: 34314735
Coddou et al (2019) Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor. Neurosci Lett 690 219 PMID: 30366010
Conley (2017) Imaging extracellular ATP with a genetically-encoded, ratiometric fluorescent sensor. PLoS One 12 e0187481 PMID: 29121644
Mungenast (2011) Diacylglycerol signaling underlies astrocytic ATP release. Neural Plast 2011 537659 PMID: 21826278
Zhong et al (2001) Multiple P2X receptors on guinea-pig pelvic ganglion neurons exhibit novel pharmacological properties. Br J Pharmacol 132 221 PMID: 11156581
Liu et al (1999) Rat chromaffin cells lack P2X receptors while those of the guinea-pig express a P2X receptor with novel pharmacology. Br J Pharmacol 128 61 PMID: 10498835
Gao et al (1999) Evidence that the ATP-induced increase in vasomotion of guinea-pig mesenteric lymphatics involves an endothelium-dependent release of thromboxane A2. Br J Pharmacol 127 1597 PMID: 10455315
Dowd et al (1998) P2X receptor-mediated excitation of nociceptive afferents in the normal and arthritic rat knee joint. Br J Pharmacol 125 341 PMID: 9786507
Neal et al (1998) Modulation of extracellular GABA levels in the retina by activation of glial P2X-purinoceptors. Br J Pharmacol 124 317 PMID: 9641548
Zhong et al (1998) Pharmacological and molecular characterization of P2X receptors in rat pelvic ganglion neurons. Br J Pharmacol 125 771 PMID: 9831914
Dowd et al (1998) Adenosine A1 receptor-mediated excitation of nociceptive afferents innervating the normal and arthritic rat knee joint. Br J Pharmacol 125 1267 PMID: 9863656
Takata and Hirase Cortical layer 1 and layer 2/3 astrocytes exhibit distinct calcium dynamics in vivo. PLoS One 3 e2525 PMID: 18575586
Kennedy et al (2007) Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder. J Neurosci 27 845 PMID: 17251425
Do you know of a great paper that uses PPADS tetrasodium salt from Tocris? Please let us know.
Reviews for PPADS tetrasodium salt
Average Rating: 4.5 (Based on 2 Reviews.)
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Blocker of P2X channels.
By
Anonymous on 08/03/2021
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Cortical neurons
Study calcium oscillations using Fura2-AM in neuronal cultures at 10 micromolar concentration.
P2X antagonist.
By
Anonymous on 10/02/2018
Assay Type: In Vitro
Species: Mouse
used to abrogate P2X responses, worked as expected.
Literature in this Area
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P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.