PD123319

製品コードS7098 バッチS709803

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₁H₃₂N₄O₃
	分子量	508.61	CAS No.	130663-39-7
Solubility (25°C)*	体外	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.

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生物活性

製品説明	PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 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]

プロトコル(参考用のみ)

動物実験	動物モデル	spontaneously hypertensive rats
	投薬量	0.36 and 1 mg/kg/min
	投与方法	intravenous

参考

[4] Tamura M, et al. J Hypertens, 2000, 18(9), 1239-1246.

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カスタマーフィードバック

: , , 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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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