Overview
Alternative Name CHEMBL157946, PD 123319 (ditrifluoroacetate), PD 123319 di(trifluoroacetate), PD 123,319 di(trifluoroacetate) salt hydrate
Lyophilized Powder yes
Source Synthetic
MW: 736.66
Purity: ≥97%
Effective concentration 1 nM – 10 µM.
Structure
Chemical name (6S)-1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-6,7-dihydro-4H-imidazo[4,5-c]pyridine-6-carboxylic acid;2,2,2-trifluoroacetic acid.
Molecular formula C35H34F6N4O7.
CAS No.: 136676-91-0
PubChem CID 6604951
Activity An Angiotensin II Type 2 Receptor Antagonist1,2.
References-Activity
- Blankley, C.J. et al. (1991) J. Med. Chem. 34, 3248.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility 100 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C.
Our bioassay
Alomone Labs PD 123319 ditrifluoroacetate inhibits specific binding of CGP-42112A to human recombinant angiotensin AT2 receptors expressed in CHO-K1 cells.Percent inhibition of specific binding of 0.05 nM [125I] CGP-42112A to CHO-K1 cells expressing human recombinant angiotensin AT2 receptors was plotted against concentrations of PD 123319 ditrifluoroacetate (#P-245), (green circles) and of Saralasin (assay standard, black squares) and used to calculate IC50 and Ki values for PD 123319 ditrifluoroacetate (IC50 ≈ 5.09 nM, and Ki ≈ 2.26 nM).
Scientific background
PD 123319 ditrifluoroacetate is a potent and selective antagonist of Angiotensin II type 2 receptor (AT2R) with an IC50 value of 34 nM3. It is also a weak Angiotensin II type 1 receptor antagonist. PD 123319 blocks the activation of the receptor by angiotensin II (Ang II), a natural hormone produced in order to maintain normal regulation of the cardiovascular function1.
Blocking the angiotensin system has an important role in preventing progressive renal dysfunction and cardiovascular morbidity and mortality by reducing blood pressure and proteinuria. Ang II receptor antagonists are useful tools for treatment of chronic kidney disease in diabetic and non-diabetic patients2.
Target AT2R receptors
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
Citations
