[CAS NO. 136676-91-0] PD 123319 ditrifluoroacetate
PRODUCTS SPECIFICATIONS [136676-91-0]
DESCRIPTION [136676-91-0]
Overview
| MDL | MFCD08276969 |
|---|---|
| Molecular Weight | 736.66 |
| Molecular Formula | C35H34F6N4O7 |
| SMILES | FC(F)(C(O)=O)F.FC(F)(C(O)=O)F.O=C([C@@H]1CC2=C(N=CN2CC3=CC=C(N(C)C)C(C)=C3)CN1C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)O |
8 Publications Citing Use of MCE
- [1]J Exp Med. 2022 Mar 7;219(3):e20211001.
- [2]Redox Biol. October 2021, 102115.
- [3]FASEB J. 2019 May;33(5):6254-6268.
- [4]FASEB J. 2018 Sep;32(9):5051-5062.
- [5]Int Immunopharmacol. 2022 Jun 17;110:108921.
- [6]SSRN. 13 Apr 2022.
- [7]Rep Biochem Mol Biol. 2021 Jul;10(2):314-326.
- [8]Reports of Biochemistry and Molecular Biology. 2021 Aug.
Summary
PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC 50 of 34 nM.
IC50 & Target
IC50: 34 nM (AT2 Receptor) [1]
In Vitro
PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues. 125 I-AII specifically label 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 (IC 50 of 92.9 nM) for DuP-753. PD-123319 does not have any effect on 125 I-AII binding to this site. The second class of binding sites is more sensitive to PD-123319, with an IC 50 of 6.9 nM, and has a much lower affinity for DuP-753 (IC 50 around 10 microM) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : ≥ 36 mg/mL ( 48.87 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.3575 mL | 6.7874 mL | 13.5748 mL |
| 5 mM | 0.2715 mL | 1.3575 mL | 2.7150 mL |
| 10 mM | 0.1357 mL | 0.6787 mL | 1.3575 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (135.75 mM); Clear solution; Need ultrasonic
References
- [1] 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.
- [2] 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
- [3] 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.
- [4] Brillante DG, et al. Effects of intravenous PD 123319 on haemodynamic and arterial stiffness indices in healthy volunteers. J Renin Angiotensin Aldosterone Syst. 2005 Sep;6(2):102-6.
