PD-123319 TFA salt
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MedKoo CAT#: 526641

CAS#: 136676-91-0 (TFA)

Description: 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 Structure

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PD-123319 TFA salt
CAS# 136676-91-0 (TFA)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526641
Name: PD-123319 TFA salt
CAS#: 136676-91-0 (TFA)
Chemical Formula: C35H34F6N4O7
Exact Mass: 0.00
Molecular Weight: 736.668
Elemental Analysis: C, 57.07; H, 4.65; F, 15.47; N, 7.61; O, 15.20

Price and Availability

Size Price Availability Quantity
5mg USD 285 2 Weeks
10mg USD 505 2 Weeks
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Related CAS #: 136676-91-0 (TFA)   130663-39-7 (free base),  

Synonym: PD-123319; PD 123319; PD123319; PD-123319 TFA; PD 123319 ditrifluoroacetate.

IUPAC/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 compound with 2,2,2-trifluoroacetic acid (1:2)

InChi Key: GPKQIEZLHVGJQH-ZXVJYWQYSA-N

InChi Code: InChI=1S/C31H32N4O3.2C2HF3O2/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;2*3-2(4,5)1(6)7/h4-16,20,28-29H,17-19H2,1-3H3,(H,37,38);2*(H,6,7)/t28-;;/m0../s1

SMILES Code: O=C([C@H]1N(CC2=C(C1)N(C=N2)CC3=CC=C(C(C)=C3)N(C)C)C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)O.FC(C(O)=O)(F)F.FC(C(O)=O)(F)F

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, not in water

Shelf Life: >2 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

More Info: Related CAS# CAS#130663-39-7 (PD-123319 free base). CAS#136676-91-0 (PD-123319 TFA)

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
In vitro activity: Human MSCs were differentiated into osteoblasts. Expression of AT2R was significantly increased during osteogenesis, whereas the expression of Ang II type 1 receptors was not significantly changed. Incubation with the AT2R blocker PD123319 with or without Ang II significantly inhibited calcium deposition, whereas type 1 receptor blocker valsartan had no significant effect. PD123319 inhibited extracellular signal-regulated kinase (ERK) phosphorylation in the osteogenic process, whereas valsartan had no effect. Furthermore, PD123319 combined with Ang II also inhibited acute ERK phosphorylation in MSCs induced by insulin. Reference: J Am Soc Hypertens. 2015 Jul;9(7):517-25. https://pubmed.ncbi.nlm.nih.gov/26188399/
In vivo activity: This study aimed to determine the effects of losartan and PD123319 in ischemia-reperfusion (IR) injury in isolated perfused rat heart. A partial recovery of cardiodynamic parameters was observed in all treatment groups. A significant increase in oxidative stress parameters were seen in the IR group, whereas all treatment groups exhibited lower increase. Furthermore, levels of all antioxidant parameters were significantly lower in the IR group, but higher in the treatment groups. Effects on all parameters were much more remarkable in the PD123319 group. Reference: Can J Physiol Pharmacol. 2019 Dec;97(12):1124-1131. https://pubmed.ncbi.nlm.nih.gov/31361968/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 30.0 40.72
DMSO 25.0 33.94
Ethanol 30.0 40.72
PBS (pH 7.2) 10.0 13.57
Water 43.5 59.09

Preparing Stock Solutions

The following data is based on the product molecular weight 736.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Matsushita K, Wu Y, Pratt RE, Dzau VJ. Blockade of angiotensin II type 2 receptor by PD123319 inhibits osteogenic differentiation of human mesenchymal stem cells via inhibition of extracellular signal-regulated kinase signaling. J Am Soc Hypertens. 2015 Jul;9(7):517-25. doi: 10.1016/j.jash.2015.06.006. Epub 2015 Jun 12. PMID: 26188399. 2. 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. 3. 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.
In vitro protocol: 1. Matsushita K, Wu Y, Pratt RE, Dzau VJ. Blockade of angiotensin II type 2 receptor by PD123319 inhibits osteogenic differentiation of human mesenchymal stem cells via inhibition of extracellular signal-regulated kinase signaling. J Am Soc Hypertens. 2015 Jul;9(7):517-25. doi: 10.1016/j.jash.2015.06.006. Epub 2015 Jun 12. PMID: 26188399.
In vivo protocol: 1. 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. 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.

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This message contains search results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM). Do not reply directly to this message

Sent On: Wed Oct 21 16:17:15 2020

Search: PD123319 [title]

18 selected items


PubMed Results
Items 1-18 of 18 (Display the 18 citations in PubMed)

1: 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.


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: 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.


4: 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.


5: Matsushita K, Wu Y, Pratt RE, Dzau VJ. Blockade of angiotensin II type 2 receptor by PD123319 inhibits osteogenic differentiation of human mesenchymal stem cells via inhibition of extracellular signal-regulated kinase signaling. J Am Soc Hypertens. 2015 Jul;9(7):517-25. doi: 10.1016/j.jash.2015.06.006. Epub 2015 Jun 12. PMID: 26188399.


6: Wagenaar GT, Sengers RM, Laghmani el H, Chen X, Lindeboom MP, Roks AJ, Folkerts G, Walther FJ. Angiotensin II type 2 receptor ligand PD123319 attenuates hyperoxia-induced lung and heart injury at a low dose in newborn rats. Am J Physiol Lung Cell Mol Physiol. 2014 Aug 1;307(3):L261-72. doi: 10.1152/ajplung.00345.2013. Epub 2014 Jun 20. PMID: 24951776; PMCID: PMC4121644.


7: Daugherty A, Rateri DL, Howatt DA, Charnigo R, Cassis LA. PD123319 augments angiotensin II-induced abdominal aortic aneurysms through an AT2 receptor- independent mechanism. PLoS One. 2013 Apr 12;8(4):e61849. doi: 10.1371/journal.pone.0061849. PMID: 23593499; PMCID: PMC3625148.


8: Jones ES, Black MJ, Widdop RE. Influence of Angiotensin II Subtype 2 Receptor (AT(2)R) Antagonist, PD123319, on Cardiovascular Remodelling of Aged Spontaneously Hypertensive Rats during Chronic Angiotensin II Subtype 1 Receptor (AT(1)R) Blockade. Int J Hypertens. 2012;2012:543062. doi: 10.1155/2012/543062. Epub 2012 Mar 4. PMID: 22500216; PMCID: PMC3303759.


9: Gilles R, Vingerhoedt N, Howes J, Griffin M, Howes LG. Increase in systemic blood pressure during intra-arterial PD123319 infusion: evidence for functional expression of angiotensin type 2 receptors in normal volunteers. Blood Press. 2004;13(2):110-4. doi: 10.1080/08037050310031017. PMID: 15182114.


10: Georgiev V, Opitz M. Participation of angiotensin receptors in acute hypoxia in mice. II. Effects of angiotensin II nonpeptide receptor ligands losartan (DuP-753) and PD-123319. Methods Find Exp Clin Pharmacol. 1999 Sep;21(7):463-6. PMID: 10544388.


11: Bivalacqua TJ, Dalal A, Lambert DG, Champion HC, Kadowitz PJ. Effects of candesartan and PD123319 on responses to angiotensin II in the anesthetized mouse. J Am Soc Nephrol. 1999 Jan;10 Suppl 11:S98-100. PMID: 9892148.


12: Champion HC, Bivalacqua TJ, Lambert DG, McNamara DB, Kadowitz PJ. The influence of candesartan and PD123319 on responses to angiotensin II in the hindquarters vascular bed of the rat. J Am Soc Nephrol. 1999 Jan;10 Suppl 11:S95-7. PMID: 9892147.


13: Mikuni M, Brännström M, Hellberg P, Peterson CA, Pall M, Edwin SS, Peterson CM. Saralasin-induced inhibition of ovulation in the in vitro perfused rat ovary is not replicated by the angiotensin II type-2 receptor antagonist PD123319. Am J Obstet Gynecol. 1998 Jul;179(1):35-40. doi: 10.1016/s0002-9378(98)70248-0. PMID: 9704762.


14: Ling Q, Guo Z, Chen T, Yu Y. Effects of losartan and PD123319 on antigensin II-induced proto-oncogene expression and protein synthesis in cultured neonatal rat cardiac myocytes. Hunan Yi Ke Da Xue Xue Bao. 1997;22(4):283-6. PMID: 9868075.


15: do-Prado MH, Camargo GM, Renzi A, Saad WA, Luiz AC, Queiróz RC, Camargo LA. Paraventricular nucleus administration of DuP753 or PD123319 inhibits the effects of angiotensin on water and sodium intake. Braz J Med Biol Res. 1996 Nov;29(11):1499-502. PMID: 9196552.


16: De Luca LA Jr, Barbosa SP, Sugawara AM, Menani JV. Effects of intracerebroventricular injections of losartan or PD123319 on arterial pressure and heart rate of sodium replete and sodium deplete rats. Regul Pept. 1996 Oct 8;66(1-2):31-5. doi: 10.1016/0167-0115(96)00055-9. PMID: 8899889.


17: Cervenka L, Heller J, Jelínek F. Lack of a beneficial effect of PD123319, an AT2-angiotensin receptor antagonist, on the course of ablation nephropathy in the rat. Kidney Blood Press Res. 1996;19(5):241-4. doi: 10.1159/000174082. PMID: 8956235.


18: Nossaman BD, Feng CJ, Kaye AD, Kadowitz PJ. Analysis of responses to ANG IV: effects of PD-123319 and DuP-753 in the pulmonary circulation of the rat. Am J Physiol. 1995 Feb;268(2 Pt 1):L302-8. doi: 10.1152/ajplung.1995.268.2.L302. PMID: 7864150.