PD-123319 free base

PD-123319 is a selective, nonpeptide AT2R antagonist (IC50 = 5.6 nM vs. 100 nM for AT1R). PD-123319 has been used to selectively examine the specific roles for AT1R and AT2R in hypertensive and other vascular research-related models..

Product information

CAS Number: 130663-39-7

Molecular Weight: 508.61

Formula: C31H32N4O3

Synonym:

PD 123319

PD123319

PD-123319 free base

Chemical Name:  (S)-1-(4-(dimethylamino)-3-methylbenzyl)-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid

Smiles: CN(C)C1=CC=C(CN2C=NC3CN([C@@H](CC2=3)C(O)=O)C(=O)C(C2C=CC=CC=2)C2C=CC=CC=2)C=C1C

InChiKey: YSTVFDAKLDMYCR-NDEPHWFRSA-N

InChi: InChI=1S/C31H32N4O3/c1-21-16-22(14-15-26(21)33(2)3)18-34-20-32-25-19-35(28(31(37)38)17-27(25)34)30(36)29(23-10-6-4-7-11-23)24-12-8-5-9-13-24/h4-16,20,28-29H,17-19H2,1-3H3,(H,37,38)/t28-/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

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 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).

References:

1. Muñoz MC, Burghi V, Miquet JG, Cervino IA, Quiroga DT, Mazziotta L, Dominici FP. Chronic blockade of the AT2 receptor with PD123319 impairs insulin signaling in C57BL/6 mice. Peptides. 2017 Feb;88:37-45. doi: 10.1016/j.peptides.2016.12.003. Epub 2016 Dec 12. PMID: 27979738.
2. Zizzo MG, Caldara G, Bellanca A, Nuzzo D, Di Carlo M, Serio R. PD123319, angiotensin II type II receptor antagonist, inhibits oxidative stress and inflammation in 2, 4-dinitrobenzene sulfonic acid-induced colitis in rat and ameliorates colonic contractility. Inflammopharmacology. 2020 Feb;28(1):187-199. doi: 10.1007/s10787-019-00619-z. Epub 2019 Jul 18. PMID: 31321575.
3. Ying X, Kai-Pan G, Wei-Qing L, Long-Yun P, De-Xi W, Zhi-Bin H. Long-term treatment of spontaneously hypertensive rats with PD123319 and electrophysiological remodeling of left ventricular myocardium. Naunyn Schmiedebergs Arch Pharmacol. 2016 Dec;389(12):1333-1340. doi: 10.1007/s00210-016-1300-0. Epub 2016 Sep 14. PMID: 27629578.

Products are for research use only. Not for human use.