PD-123319-ditrifluoroacetate - Angiotensin Receptor Antagonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPD 123319 ditrifluoroacetateCat. No.: HY-10259ACAS No.: 136676-91-0分式: CHFNO分量: 736.66作靶點(diǎn): Angiotensin Receptor作通路: GPCR/G Protein儲存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶

2、解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 36 mg/mL (48.87 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.3575 mL 6.7874 mL 13.5748 mL5 mM 0.2715 mL 1.3575 mL 2.7150 mL10 mM 0.1357 mL 0.6787 mL 1.3575 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 PD 123319

3、 ditrifluoroacetate種有效的，選擇性的 AT2 angiotensin II receptor 拮抗劑，IC50 值為 34nM。IC50 & Target IC50: 34 nM (AT2 Receptor) 1體外研究PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues. 125I-AII specifically label two classes of binding sites for AII in a membrane

4、 preparation of bovine adrenal1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEglomerulosa cells. The first class (DuP-753 sensitive) represents approximately 85% of the total binding sitesfor AII and possesses a high affinity (IC50 of 92.9 nM) for DuP-753. PD-123319 does not have any effecton 125I-

5、AII binding to this site. The second class of binding sites is more sensitive to PD-123319, with anIC50 of 6.9 nM, and has a much lower affinity for DuP-753 (IC50 around 10 microM) 2.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) FASEB J. 2019 May;33(5):6254-6268. FASEB J. 2018 Sep;32(9):5051-5062.See more customer validations on HYP

6、ERLINK / www.MedChemEREFERENCES1. Blankley CJ, et al. Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitorsspecific for the AT2 subtype. J Med Chem. 1991 Nov;34(11):3248-60.2. Boulay G, et al. Modulation of angiotensin II binding a

7、ffinity by allosteric interaction of polyvinyl sulfate with an intracellular domain of theDuP-753-sensitive angiotensin II receptor of bovine adrenal glomerulosa. Mol Pharmacol. 1992 Apr;41(4):809-153. Estrup TM, et al. No effect of angiotensin II AT(2)-receptor antagonist PD 123319 on cerebral bloo

8、d flow autoregulation. J ReninAngiotensin Aldosterone Syst. 2001 Sep;2(3):188-92.4. Brillante DG, et al. Effects of intravenous PD 123319 on haemodynamic and arterial stiffness indices in healthy volunteers. J ReninAngiotensin Aldosterone Syst. 2005 Sep;6(2):102-6.McePdfHeightCaution: Product has not been fully validated for medical applications.F