受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C31H32N4O3 |
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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. |
製品説明 | PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. |
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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] |
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] |
動物実験 | 動物モデル | spontaneously hypertensive rats |
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投薬量 | 0.36 and 1 mg/kg/min | |
投与方法 | intravenous |
, , 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]
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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