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PPADS tetrasodium salt is a novel and potent P2X receptor antagonist P2X receptor antagonist that blocks recombinant P2X1, -2, -3, -5 with IC50s in the range of 1 to 2.6 μM.
ln Vitro |
Na+/Ca2+ exchanger reverse mode (NCXREV) is inhibited by PPADS tetrasodiuma (1-30 μM; 10-50 min) in a concentration- and time-dependent manner [2]. Tetrasodium PPADS is efficient against recombinant and other native P2XRs. Human P2XRs' sensitivity to PPADS tetrasodium varied depending on the subtype; the most sensitive subtypes were hP2X1, -2, -3, -5, and -7R, whereas hP2X4R had IC50s of around 1-3 and ~30 μM, respectively [3].
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ln Vivo |
Mesangial cell (MC) proliferation in vivo in mesangial proliferative nephritis is inhibited by PPADS tetrasodiuma (15–60 mg/100g body weight (BW); intraperitoneal injection; every 12 hours for 8 days) without affecting non-MC in vivo proliferation [4].
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Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats, body weight 160 to 200 g (anti-Thy1 disease model) [4]
Doses: 15 mg/100g BW, 30 mg/100g BW, 60 mg/100g BW Route of Administration: intraperitoneal (ip) injection; every 12 hrs (hrs (hours)) for 8 days (The first PPADS injection was given 60 minutes after disease induction, and the loading dose always contained double the amount of PPADS compared with subsequent injections.) Experimental Results: Early (day 3) specifically And dose-dependently diminished mesangial cell proliferation without changing non-MC proliferation. |
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 |
C14H10N3O12PS2-4.4[NA+]
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Molecular Weight |
599.3051
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CAS # |
192575-19-2
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Related CAS # |
Iso-PPADS tetrasodium;207572-67-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
[Na+].[Na+].[Na+].[Na+].O=P(OCC1=C(C=O)C(=O)C(C)=N/C/1=N/NC1C=CC(S([O-])(=O)=O)=CC=1S([O-])(=O)=O)([O-])[O-]
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O : ~50 mg/mL (~83.43 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6686 mL | 8.3429 mL | 16.6859 mL | |
5 mM | 0.3337 mL | 1.6686 mL | 3.3372 mL | |
10 mM | 0.1669 mL | 0.8343 mL | 1.6686 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.