PD123319

Catalog No.S7098 Batch:S709803

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Technical Data

Formula

C31H32N4O3
Molecular Weight 508.61 CAS No. 130663-39-7
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)
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Study:[3]
  • Animal Models

    spontaneously hypertensive rats

  • Dosages

    0.36 and 1 mg/kg/min

  • Administration

    intravenous

Customer Product Validation

, , Acta Biochim Biophys Sin (Shanghai), 2015, 47(7):539-47.

, , Exp Biol Med (Maywood), 2015, 240(12):1564-71.

Data from [Data independently produced by , , Naunyn Schmiedebergs Arch Pharmacol, 2016, 389(12):1333-1340]

Selleck's PD123319 has been cited by 12 publications

Cartilage oligomeric matrix protein is an endogenous β-arrestin-2-selective allosteric modulator of AT1 receptor counteracting vascular injury [ Cell Res, 2021, 10.1038/s41422-020-00464-8] PubMed: 33510386
Angiotensin II inhibits osteogenic differentiation of isolated synoviocytes by increasing DKK-1 expression. [ Int J Biochem Cell Biol, 2020, 121:105703] PubMed: 32014499
Angiotensin II down-regulates transferrin receptor 1 and ferroportin 1 expression in Neuro-2a cells via activation of type-1 receptor. [ Neurosci Lett, 2020, 716:134684] PubMed: 31830506
(Pro)renin receptor contributes to hypoxia/reoxygenation-induced apoptosis and autophagy in myocardial cells via the beta-catenin signaling pathway [ Physiol Res, 2020, 69(3):427-438] PubMed: 32469229
Alamandine attenuates long‑term hypertension‑induced cardiac fibrosis independent of blood pressure. [ Mol Med Rep, 2019, 19(6):4553-4560] PubMed: 31059021
[ J Immunother Cancer, 2018, ] PubMed: 30208943
Role of angiotensin II type 2 receptor during electrophysiological remodeling of left ventricular hypertrophic myocardium in spontaneously hypertensive rats [Xiao Y, et al. J Am Soc Hypertens, 2018, 12(1):58-65] PubMed: 29100861
Angiotensin II induces connective tissue growth factor expression in human hepatic stellate cells by a transforming growth factor β-independent mechanism. [ Sci Rep, 2017, 7(1):7841] PubMed: 28798388
Long-term treatment of spontaneously hypertensive rats with PD123319 and electrophysiological remodeling of left ventricular myocardium. [Ying X, et al. Naunyn Schmiedebergs Arch Pharmacol, 2016, 389(12):1333-1340] PubMed: 27629578
Angiotensin II induces an increase in MMP-2 expresison in idiopathic ascending aortic aneurysm via AT1 receptor and JNK pathway. [Wang C, et al. Acta Biochim Biophys Sin, 2015, 47(7), 1–9] PubMed: 26071572

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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