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Submit ReviewPD 123319 ditrifluoroacetate
Description: Potent and selective non-peptide AT2 antagonist
Chemical Name: (6S)1-[[4-(Dimethylamino)-3-methylphenyl]methyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid ditrifluoroacetate
Purity: ≥99% (HPLC)
Biological Activity for PD 123319 ditrifluoroacetate
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.
Technical Data for PD 123319 ditrifluoroacetate
| M. Wt | 736.67 |
| Formula | C31H32N4O3.2CF3CO2H |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 136676-91-0 |
| PubChem ID | 6604951 |
| InChI Key | GPKQIEZLHVGJQH-ZXVJYWQYSA-N |
| Smiles | O=C(C(C5=CC=CC=C5)C4=CC=CC=C4)N1[C@H]([C@](O)=O)CC(N(CC3=CC(C)=C(N(C)C)C=C3)C=N2)=C2C1.FC(F)(F)C(O)=O.FC(F)(F)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PD 123319 ditrifluoroacetate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 51.06 | 100 |
Preparing Stock Solutions for PD 123319 ditrifluoroacetate
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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.36 mL | 6.79 mL | 13.57 mL |
| 5 mM | 0.27 mL | 1.36 mL | 2.71 mL |
| 10 mM | 0.14 mL | 0.68 mL | 1.36 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.27 mL |
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Product Datasheets for PD 123319 ditrifluoroacetate
References for PD 123319 ditrifluoroacetate
References are publications that support the biological activity of the product.
Blankley et al (1991) Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. J.Med.Chem. 34 3248 PMID: 1956044
Boulay et al (1992) Modulation of angiotensin II binding affinity by allosteric interaction of polyvinyl sulfate with an intracellular domain of the DuP-753-sensitive angiotensin II receptor of bovine adrenal glomerulosa. Mol.Pharmacol. 41 809 PMID: 1569928
Tamura et al (2000) Induction of angiotensin II subtype 2 receptor-mediated blood pressure regulation in synthetic diet-fed rats. J.Hypertens. 18 1239 PMID: 10994755
If you know of a relevant reference for PD 123319 ditrifluoroacetate, please let us know.
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Keywords: PD 123319 ditrifluoroacetate, PD 123319 ditrifluoroacetate supplier, Potent, selective, non-peptide, AT2, antagonists, Receptors, Angiotensin, PD123319, ditrifluoroacetate, 1361, Tocris Bioscience
22 Citations for PD 123319 ditrifluoroacetate
Citations are publications that use Tocris products. Selected citations for PD 123319 ditrifluoroacetate include:
Cruz et al (2013) High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses. PLoS Negl Trop Dis 7 e2073 PMID: 23437413
Chakrabarty et al (2013) Angiotensin II receptor type 2 activation is required for cutaneous sensory hyperinnervation and hypersensitivity in a rat hind paw model of inflammatory pain. J Pain 14 1053 PMID: 23726047
Hong and Garvin (2012) Angiotensin II type 2 receptor-mediated inhibition of NaCl absorption is blunted in thick ascending limbs from Dahl salt-sensitive rats. Diabetes 60 765 PMID: 22777935
Moreno-Santos et al (2021) 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. 397 PMID: 33011187
Nemoto et al (2013) Angiotensin II produces nociceptive behavior through spinal AT1 receptor-mediated p38 mitogen-activated protein kinase activation in mice. Mol Pain 9 38 PMID: 23898828
Bourassa et al (2010) AT1 angiotensin II receptor and novel non-AT1, non-AT2 angiotensin II/III binding site in brainstem cardiovascular regulatory centers of the spontaneously hypertensive rat. Brain Res 1359 98 PMID: 20807518
Curato et al (2010) Identification of noncytotoxic and IL-10-producing CD8+AT2R+ T cell population in response to ischemic heart injury. PLoS One 185 6286 PMID: 20935205
Benkirane et al (2006) PPAR- γ inhibits ANG II-induced cell growth via SHIP2 and 4E-BP1. Hypertension 290 H390 PMID: 16155101
Tsai et al (2012) Brain-derived neurotrophic factor ameliorates brain stem cardiovascular dysregulation during experimental temporal lobe status epilepticus. Am J Physiol Heart Circ Physiol 7 e33527 PMID: 22442695
Raffai et al (2016) Angiotensin-(1-7) selectively induces relaxation and modulates endothelium-dependent dilation in mesenteric arteries of salt-fed rats Journal of Vascular Research 53 105 PMID: 27676088
Santiago et al (2014) High molecular weight fibroblast growth factor-2 in the human heart is a potential target for prevention of cardiac remodeling. PLoS One 9 e97281 PMID: 24827991
Speth et al (2014) Distribution of non-AT1, non-AT2 binding of 125I-sarcosine1, isoleucine8 angiotensin II in neurolysin knockout mouse brains. PLoS One 9 e105762 PMID: 25147932
Speth et al (2014) Acute repeated intracerebroventricular injections of angiotensin II reduce agonist and antagonist radioligand binding in the paraventricular nucleus of the hypothalamus and median preoptic nucleus in the rat brain. Brain Res 1583 132 PMID: 25108041
Santollo et al (2014) Properly timed exposure to central ANG II prevents behavioral sensitization and changes in angiotensin receptor expression. Am J Physiol Regul Integr Comp Physiol 307 R1396 PMID: 25354729
Hasin et al (2011) Angiotensin II signaling up-regulates the immediate early transcription factor ATF3 in the left but not the right atrium. Basic Res Cardiol 106 175 PMID: 21191795
Santiago et al (2011) Preferential accumulation and export of high molecular weight FGF-2 by rat cardiac non-myocytes. Cardiovasc Res 89 139 PMID: 20696821
Dominska et al (2018) Angiotensin 1-7 modulates molecular and cellular processes central to the pathogenesis of prostate cancer. Sci.Rep. 8 15772 PMID: 30361641
Gu et al (2016) Angiotensin-converting enzyme 2 inhibits lung injury induced by respiratory syncytial virus. J Immunol 6 19840 PMID: 26813885
Fan et al (2015) Local renin-angiotensin system regulates hypoxia-induced vascular endothelial growth factor synthesis in mesenchymal stem cells. Nat Commun 8 2505 PMID: 26045756
Chang et al (2015) Vasculopathy-associated hyperangiotensinemia mobilizes haematopoietic stem cells/progenitors through endothelial AT2R and cytoskeletal dysregulation. Sci Rep 6 5914 PMID: 25574809
Porter et al (2015) The angiotensin converting enzyme inhibitor, captopril, prevents the hyperactivity and impulsivity of neurokinin-1 receptor gene 'knockout' mice: sex differences and implications for the treatment of attention deficit hyperactivity disorder. Eur Neuropsychopharmacol 25 512 PMID: 25703442
Skorska et al (2015) The CD4(+) AT2R(+) T cell subpopulation improves post-infarction remodelling and restores cardiac function. J Cell Mol Med 19 1975 PMID: 25991381
Do you know of a great paper that uses PD 123319 ditrifluoroacetate from Tocris? Please let us know.
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Selective angiotensin receptor type 1 and 2 blocker PD123319 and EMD66684.
By
Hitesh Soni on 01/04/2018
Assay Type: In Vitro
Species: Other
Cell Line/Tissue: primary kidney mesangial cells
To inhibit angiotensin II receptor type1 in neonatal pig glomerular mesangial cells (primary culture) to study proliferation of mesangial cells and calcium imaging studies.
We have also used Tocris another product EMD66684 (angiotensin receptor type 2 blocker) and published results in EXPERIMENTAL CELL RESEARCH 324(2014)92 – 104.
