PD123319
For research use only.
Catalog No.S7098
11 publications
CAS No. 130663-39-7
PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
3 Customer Reviews
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Ang II-induced MMP-2 protein expression through AT1 receptor in ex vivo cultured IAAA aortic walls (A) Ex vivo cultured aortic pieces from IAAA patients (n = 5) were incubated in the presence of different concentrations of Ang II for 48 h. (B) Ex vivo cultured aneurysmal aorta walls were pre-treated with either candesartan (10 µM, AT1R inhibitor) or PD123319 (10 µM, AT2R antagonist) for 48 h, followed by 1 µM Ang II treatment for 48 h. The group without Ang II incubation was used as control. **P < 0.01 vs. untreated control group; ##P < 0.01 vs. treated with Ang II alone. CA, candesartan; PD, PD123319.
Acta Biochim Biophys Sin (Shanghai), 2015, 47(7):539-47.. PD123319 purchased from Selleck.
Ang II induces MMP-2 protein expression and ERK phosphorylation ASMCs via AT1R. (a) ASMCs were pretreated with 0.1 μM candesartan (CA, selective AT1R inhibitor, 30 min) or 1 μM PD123319 (PD, selective AT2R inhibitor, 30 min) followed by stimulation with 0.1 μM Ang II for 2 min six-well plates. Western blot was performed to assess the levels of ERK phosphorylation in cell lysates. Top panel: Graphs show the relative p-ERK1/2 protein levels, respectively, normalized to total ERK1/2 relative to control. Bottom panel: Ratio of p-ERK1/2/t-ERK1/2 protein expression, respectively, evaluated using Western blot analysis from a representative experiment. Shown are mean±SEM of three individual experiments. **P < 0.01 vs. untreated control cells; ##P < 0.01 vs. cells treated with Ang II. (b) ASMCs were incubated with 1 μM candesartan or 10 μM PD123319 for 60 min before stimulation with 0.1 μM Ang II for 24 h in six-well plates. Western blot was used for analyses of the levels of MMP-2 expression in cell lysates. Top panel: Graphs show the relative MMP-2 protein levels normalized to GAPDH relative to control. Bottom panel: Ratio of MMP-2/GAPDH protein expression from a representative Western blot experiment. Shown are mean±SEM of three individual experiments. **P < 0.01 vs. untreated control cells; ##P < 0.01 vs. cells treated with Ang II.
Exp Biol Med (Maywood), 2015, 240(12):1564-71. . PD123319 purchased from Selleck.
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Effect of PD123319 treatment on sodium current (INa). Typical recordings of INa in cells from control (a), non-PD123319 (b), and PD123319 (c). x-axis: time (ms mini-second); y-axis: current volume (pA). The voltage clamp protocol is shown in (d). e Average I-V relationships of INa density (pA/pF) as a function of step potential (mV), obtained in control (filled squares), non-PD123319 (empty squares), and PD123319 (empty circles)
Naunyn Schmiedebergs Arch Pharmacol, 2016, 389(12):1333-1340. PD123319 purchased from Selleck.
Purity & Quality Control
Choose Selective Angiotensin Receptor Inhibitors
Biological Activity
| Description | PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. | ||
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| Targets |
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| In vitro |
PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues. 125I-AII specifically labeled two classes of binding sites for AII in a membrane preparation of bovine adrenal glomerulosa cells. The first class (DuP-753 sensitive) represents approximately 85% of the total binding sites for AII and possesses a high affinity (IC50 of 92.9 nM) for DuP-753. PD-123319 does not have any effect on 125I-AII binding to this site. The second class of binding sites is more sensitive to PD-123319, with an IC50 of 6.9 nM, and has a much lower affinity for DuP-753 (IC50 around 10 microM). [2] |
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| In vivo | PD 123319 has no effect on cerebral blood flow autoregulation. Acute AT2-receptor blockade does not influence CBF autoregulation. [3]Intravenous administration of PD 123319 to conscious hypertensive rats elicites an immediate dose-dependent increase in MAP that is sustained for approximately 7.4 min with 3 mg/kg PD 123319. [4] |
Protocol
| Animal Research:[3] |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (196.61 mM) |
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| Water | 100 mg/mL (196.61 mM) | |
| Ethanol | 100 mg/mL (196.61 mM) | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): Saline For best results, use promptly after mixing. |
30 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 508.61 |
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| Formula | C31H32N4O3 |
| CAS No. | 130663-39-7 |
| Storage |
powder in solvent |
| Synonyms | N/A |
| Smiles | CC1=C(C=CC(=C1)CN2C=NC3=C2CC(N(C3)C(=O)C(C4=CC=CC=C4)C5=CC=CC=C5)C(=O)O)N(C)C |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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