Home GPCR & G Protein Angiotensin Receptor antagonist PD123319 For research use only.

PD123319

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

PD123319 Chemical Structure

PD123319 Chemical Structure

CAS No. 130663-39-7

Purity & Quality Control

PD123319 Related Products

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

Chemical Information & Solubility

Molecular Weight 508.61 Formula

C31H32N4O3
CAS No. 130663-39-7 SDF Download PD123319 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (196.61 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL


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In vivo
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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.

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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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