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..


Price and Availability

Size Price Shipping out time Quantity
100mg USD 1450 2 Weeks
200mg USD 2150 2 Weeks
500mg USD 2950 2 Weeks
1g USD 3950 2 Weeks
2g USD 5650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-27. Prices are subject to change without notice.

PD-123319 TFA salt, purity > 98%, is in stock.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526641
Name: PD-123319 TFA salt
CAS#: 136676-91-0 (TFA)
Chemical Formula: C35H34F6N4O7
Exact Mass:
Molecular Weight: 736.6684
Elemental Analysis: C, 57.07; H, 4.65; F, 15.47; N, 7.61; O, 15.20


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


Technical Data

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


Additional Information

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


References

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.