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MedKoo Cat#: 555869 | Name: PD-123319 free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

PD-123319 free base
PD-123319 free base
CAS#130663-39-7 (free base)

Theoretical Analysis

MedKoo Cat#: 555869

Name: PD-123319 free base

CAS#: 130663-39-7 (free base)

Chemical Formula: C31H32N4O3

Exact Mass: 508.2474

Molecular Weight: 508.62

Elemental Analysis: C, 73.21; H, 6.34; N, 11.02; O, 9.44

Price and Availability

Size Price Availability Quantity
50mg USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,650.00 2 Weeks
500mg USD 3,450.00 2 Weeks
1g USD 5,450.00 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 free base;
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
InChi Key
YSTVFDAKLDMYCR-NDEPHWFRSA-N
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
SMILES Code
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
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
More Info
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/
Solvent mg/mL mM
Solubility
Water 100.0 196.61
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 508.62 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.
1: Olschewski DN, Nazarzadeh N, Lange F, Koenig AM, Kulka C, Abraham JA, Blaschke SJ, Merkel R, Hoffmann B, Fink GR, Schroeter M, Rueger MA, Vay SU. The angiotensin II receptors type 1 and 2 modulate astrocytes and their crosstalk with microglia and neurons in an in vitro model of ischemic stroke. BMC Neurosci. 2024 Jun 26;25(1):29. doi: 10.1186/s12868-024-00876-x. PMID: 38926677; PMCID: PMC11202395. 2: Tang J, Lu H, Xie Z, Jia X, Su T, Lin B. Identification of potential biomarkers for sepsis based on neutrophil extracellular trap-related genes. Diagn Microbiol Infect Dis. 2024 Sep;110(1):116380. doi: 10.1016/j.diagmicrobio.2024.116380. Epub 2024 Jun 1. PMID: 38852219. 3: Peluso AA, Souza-Silva IM, Villela DC, Hansen PBL, Hallberg A, Bader M, Santos R, Sumners C, Steckelings UM. Functional assay for assessment of agonistic or antagonistic activity of angiotensin AT2 receptor ligands reveals that EMA401 and PD123319 have agonistic properties. Biochem Pharmacol. 2023 Oct;216:115793. doi: 10.1016/j.bcp.2023.115793. Epub 2023 Sep 7. PMID: 37689272. 4: Guimarães-Nobre CC, Mendonça-Reis E, Passinho-da-Costa L, Miranda-Alves L, Clemilson Berto-Junior H. Signaling Pathway in the Osmotic Resistance Induced by Angiotensin II AT2 Receptor Activation in Human Erythrocytes. Rep Biochem Mol Biol. 2021 Jul;10(2):314-326. doi: 10.52547/rbmb.10.2.314. PMID: 34604421; PMCID: PMC8480296. 5: Hossain E, Li Y, Anand-Srivastava MB. Angiotensin II-induced overexpression of sirtuin 1 contributes to enhanced expression of Giα proteins and hyperproliferation of vascular smooth muscle cells. Am J Physiol Heart Circ Physiol. 2021 Sep 1;321(3):H496-H508. doi: 10.1152/ajpheart.00898.2020. Epub 2021 Jul 16. PMID: 34270373. 6: Zhang L, Zhang B, Yu Y, Wang J, Wu J, Su Y, Jiang H, Zou Y, Ge J. Angiotensin II Increases HMGB1 Expression in the Myocardium Through AT1 and AT2 Receptors When Under Pressure Overload. Int Heart J. 2021 Jan 30;62(1):162-170. doi: 10.1536/ihj.20-384. Epub 2021 Jan 16. PMID: 33455985. 7: Borghi F, Morais CL, Silva C, da Silva PC, Grassi-Kassisse DM. The influence of angiotensin II and RAAS blockers on lipolytic and glycolytic activity in isolated adipocytes from Wistar, Wistar-Kyoto and Spontaneously Hypertensive Rats. Mol Cell Endocrinol. 2021 Jan 15;520:111086. doi: 10.1016/j.mce.2020.111086. Epub 2020 Nov 19. PMID: 33221332. 8: Moreno-Santos B, Marchi-Coelho C, Costa-Ferreira W, Crestani CC. Angiotensinergic receptors in the medial amygdaloid nucleus differently modulate behavioral responses in the elevated plus-maze and forced swimming test in rats. Behav Brain Res. 2021 Jan 15;397:112947. doi: 10.1016/j.bbr.2020.112947. Epub 2020 Oct 1. PMID: 33011187. 9: Piotrowska A, Chmielewska M, Andrzejewski W, Dziegiel P, Podhorska-Okolow M. Influence of Angiotensin II on cell viability and apoptosis in rat renal proximal tubular epithelial cells in in vitro studies. J Renin Angiotensin Aldosterone Syst. 2020 Jul-Sep;21(3):1470320320949850. doi: 10.1177/1470320320949850. PMID: 32962526; PMCID: PMC7649907. 10: Macedo LM, de Ávila RI, Pedrino GR, Colugnati DB, Valadares MC, Lima EM, Borges CL, Kitten GT, Gava E, Castro CH. Effect of angiotensin II and angiotensin-(1-7) on proliferation of stem cells from human dental apical papilla. J Cell Physiol. 2021 Jan;236(1):366-378. doi: 10.1002/jcp.29862. Epub 2020 Jun 9. PMID: 32519379. 11: Li XC, Zhou X, Zhuo JL. Evidence for a Physiological Mitochondrial Angiotensin II System in the Kidney Proximal Tubules: Novel Roles of Mitochondrial Ang II/AT1a/O2- and Ang II/AT2/NO Signaling. Hypertension. 2020 Jul;76(1):121-132. doi: 10.1161/HYPERTENSIONAHA.119.13942. Epub 2020 Jun 1. PMID: 32475319; PMCID: PMC7299167. 12: Royea J, Lacalle-Aurioles M, Trigiani LJ, Fermigier A, Hamel E. AT2R's (Angiotensin II Type 2 Receptor's) Role in Cognitive and Cerebrovascular Deficits in a Mouse Model of Alzheimer Disease. Hypertension. 2020 Jun;75(6):1464-1474. doi: 10.1161/HYPERTENSIONAHA.119.14431. Epub 2020 May 4. PMID: 32362228. 13: Friederich-Persson M, Persson P. Mitochondrial angiotensin II receptors regulate oxygen consumption in kidney mitochondria from healthy and type 1 diabetic rats. Am J Physiol Renal Physiol. 2020 Mar 1;318(3):F683-F688. doi: 10.1152/ajprenal.00417.2019. Epub 2020 Jan 6. PMID: 31904285. 14: Zhu Y, Cui H, Lv J, Liang H, Zheng Y, Wang S, Wang M, Wang H, Ye F. AT1 and AT2 receptors modulate renal tubular cell necroptosis in angiotensin II-infused renal injury mice. Sci Rep. 2019 Dec 19;9(1):19450. doi: 10.1038/s41598-019-55550-8. PMID: 31857626; PMCID: PMC6923374. 15: Kim HJ, Jang JH, Zhang YH, Yoo HY, Kim SJ. Fast relaxation and desensitization of angiotensin II contraction in the pulmonary artery via AT1R and Akt-mediated phosphorylation of muscular eNOS. Pflugers Arch. 2019 Oct;471(10):1317-1330. doi: 10.1007/s00424-019-02305-z. Epub 2019 Aug 30. PMID: 31468138. 16: Zhang M, Lu L, Zhang Y, Li X, Fan X, Chen X, Tang J, Han B, Li M, Tao J, Gao Q, Xu Z, Sun M. Methylation-reprogrammed AGTR1 results in increased vasoconstriction by angiotensin II in human umbilical cord vessel following in vitro fertilization-embryo transfer. Life Sci. 2019 Oct 1;234:116792. doi: 10.1016/j.lfs.2019.116792. Epub 2019 Aug 26. PMID: 31465733. 17: Costa-Ferreira W, Gomes-de-Souza L, Crestani CC. AT2 and MAS (but not AT1) angiotensinergic receptors in the medial amygdaloid nucleus modulate the baroreflex activity in rats. Pflugers Arch. 2019 Sep;471(9):1173-1182. doi: 10.1007/s00424-019-02301-3. Epub 2019 Aug 8. PMID: 31396758. 18: 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. 19: 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. 20: Shepherd AJ, Mohapatra DP. Attenuation of Unevoked Mechanical and Cold Pain Hypersensitivities Associated With Experimental Neuropathy in Mice by Angiotensin II Type-2 Receptor Antagonism. Anesth Analg. 2019 Jun;128(6):e84-e87. doi: 10.1213/ANE.0000000000003857. PMID: 31094778; PMCID: PMC6652216. .268.2.L302. PMID: 7864150.