Cas：130663-39-7 (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.
Chemical Formula: C31H32N4O3
Exact Mass: 508.2474
Molecular Weight: 508.622
Elemental Analysis: C, 73.21; H, 6.34; N, 11.02; O, 9.44
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
InChi Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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).
Kilic A, Ustunova S, Usta C, Bulut H, Meral I, Demirci Tansel C, Gurel Gurevin E. Angiotensin II type 2 receptor blocker PD123319 has more beneficial effects than losartan on ischemia-reperfusion injury and oxidative damage in isolated rat heart. Can J Physiol Pharmacol. 2019 Dec;97(12):1124-1131. doi: 10.1139/cjpp-2019-0076. Epub 2019 Jul 30. PMID: 31361968.
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.
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.
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.
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