| Description | PD 123319 (ditrifluoroacetate) is a potent and selective antagonist of AT2 angiotensin II receptor(IC50 of 34 nM). |
| In vitro | PD-123319 did not have any effect on 125I-All binding to this site.?The second class of binding sites was more sensitive to PD-123319, with an IC50 of 6.9 +/- 3.7 nM, and had a much lower affinity for DuP-753 (IC50 around 10 microM).?The two classes of receptors had different affinities for All.?All showed an affinity around 2 nM for All type 1 receptor (AT1)(DuP-753 sensitive) and a higher affinity, around 0.3 nM, for All type 2 receptor (AT2) (PD-123319 sensitive).?All-induced steroidogenesis was completely abolished in the presence of 3 microM DuP-753, indicating that this activity was mediated through a DuP-753-sensitive receptor. |
| Target activity | AT2 receptor:34 nM |
| molecular weight | 736.66 |
| Molecular formula | C35H34F6N4O7 |
| CAS | 136676-91-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | H2O: 36 mg/mL (48.87 mM) |
| References | 1. Boulay G, et al. Modulation of angiotensin II binding affinity by allosteric interaction of polyvinyl sulfate with an intracellular domain of the DuP-753-sensitive angiotensin II receptor of bovine adrenal glomerulosa. Mol Pharmacol. 1992 Apr;41(4):809-15 2. Estrup TM, et al. No effect of angiotensin II AT(2)-receptor antagonist PD 123319 on cerebral blood flow autoregulation. J Renin Angiotensin Aldosterone Syst. 2001 Sep;2(3):188-92. 3. Blankley CJ, et al. Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. J Med Chem. 1991 Nov;34(11):3248-60. |