Home GPCR & G Protein Angiotensin Receptor antagonist PD123319

PD123319

Catalog No.S7098

For research use only.

PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

PD123319 Chemical Structure

CAS No. 130663-39-7

Selleck's PD123319 has been cited by 12 Publications

3 Customer Reviews

Purity & Quality Control

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Biological Activity

Description PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
Targets
AT2 receptor [1]
34 nM
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]
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 (from reference)

Animal Research:[3]
  • Animal Models: spontaneously hypertensive rats
  • Dosages: 0.36 and 1 mg/kg/min
  • Administration: intravenous

Solubility (25°C)

In vitro

 DMSO 100 mg/mL
(196.61 mM)
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

Chemical Information

Molecular Weight 508.61
Formula

C31H32N4O3
CAS No. 130663-39-7
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Molarity Calculator

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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.

Handling Instructions

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