PD 123319 ditrifluoroacetate

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1361/10
1361/50
PD 123319 ditrifluoroacetate | CAS No. 136676-91-0 | Angiotensin AT2 Receptor Antagonists
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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%

Product Details
Citations (22)
Supplemental Products
Reviews

Biological Activity

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

M.Wt:
736.67
Formula:
C31H32N4O3.2CF3CO2H
Solubility:
Soluble to 100 mM in water
Purity:
≥99%
Storage:
Store at -20°C
CAS No:
136676-91-0

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.

Background References

  1. Angiotensin II acting on brain AT1 receptors induces adrenaline secretion and pressor responses in the rat.
    Nakamura, Kumiko, Shimizu, Takahiro, Yanagita, Toshihik, Nemoto, Takayuki, Taniuchi, Keisuke, Shimizu, Shogo, Dimitriadis, Fotios, Yawata, Toshio, Higashi, Youichir, Ueba, Tetsuya, Saito, Motoaki
    Sci Rep, 2014;4(0):7248.
  2. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  3. Brain-derived neurotrophic factor ameliorates brain stem cardiovascular dysregulation during experimental temporal lobe status epilepticus.
    Tsai CY, Chan JY, Hsu KS
    PLoS ONE, 2012;7(3):e33527.
  4. Angiotensin II centrally induces frequent detrusor contractility of the bladder by acting on brain angiotensin II type 1 receptors in rats
    B Kawamoto, S Shimizu, T Shimizu, Y Higashi, M Honda, T Sejima, M Saito, A Takenaka
    Sci Rep, 2016;6(0):22213.
  5. Vasculopathy-associated hyperangiotensinemia mobilizes haematopoietic stem cells/progenitors through endothelial AT(2)R and cytoskeletal dysregulation.
    Chang K, Nayak R, Roy S, Perumbeti A, Wellendorf A, Bezold K, Pirman M, Hill S, Starnes J, Loberg A, Zhou X, Inagami T, Zheng Y, Malik P, Cancelas J
    Nat Commun, 2015;6(0):5914.
  6. Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype.
    Blankley et al.
    J.Med.Chem., 1991;34:3248
  7. 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.
    Boulay et al.
    Mol.Pharmacol., 1992;41:809
  8. Induction of angiotensin II subtype 2 receptor-mediated blood pressure regulation in synthetic diet-fed rats.
    Tamura et al.
    J.Hypertens., 2000;18:1239

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Citations for PD 123319 ditrifluoroacetate

The citations listed below are publications that use Tocris products. Selected citations for PD 123319 ditrifluoroacetate include:

22 Citations: Showing 1 - 10

  1. Angiotensinergic receptors in the medial amygdaloid nucleus differently modulate behavioral responses in the elevated plus-maze and forced swimming test in rats.
    Authors: Moreno-Santos Et al.
    Behav.Brain Res.  2021;397
  2. Angiotensin 1-7 modulates molecular and cellular processes central to the pathogenesis of prostate cancer.
    Authors: Dominska Et al.
    Sci.Rep.  2018;8:15772
  3. Angiotensin-converting enzyme 2 inhibits lung injury induced by respiratory syncytial virus.
    Authors: Gu Et al.
    J Immunol  2016;6:19840
  4. Angiotensin-(1-7) selectively induces relaxation and modulates endothelium-dependent dilation in mesenteric arteries of salt-fed rats
    Authors: Raffai Et al.
    Journal of Vascular Research  2016;53:105
  5. Local renin-angiotensin system regulates hypoxia-induced vascular endothelial growth factor synthesis in mesenchymal stem cells.
    Authors: Fan Et al.
    Nat Commun  2015;8:2505
  6. Vasculopathy-associated hyperangiotensinemia mobilizes haematopoietic stem cells/progenitors through endothelial AT2R and cytoskeletal dysregulation.
    Authors: Chang Et al.
    Sci Rep  2015;6:5914
  7. 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.
    Authors: Porter Et al.
    Eur Neuropsychopharmacol  2015;25:512
  8. The CD4(+) AT2R(+) T cell subpopulation improves post-infarction remodelling and restores cardiac function.
    Authors: Skorska Et al.
    J Cell Mol Med  2015;19:1975
  9. High molecular weight fibroblast growth factor-2 in the human heart is a potential target for prevention of cardiac remodeling.
    Authors: Santiago Et al.
    PLoS One  2014;9:e97281
  10. Distribution of non-AT1, non-AT2 binding of 125I-sarcosine1, isoleucine8 angiotensin II in neurolysin knockout mouse brains.
    Authors: Speth Et al.
    PLoS One  2014;9:e105762
  11. Properly timed exposure to central ANG II prevents behavioral sensitization and changes in angiotensin receptor expression.
    Authors: Santollo Et al.
    Am J Physiol Regul Integr Comp Physiol  2014;307:R1396
  12. 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.
    Authors: Speth Et al.
    Brain Res  2014;1583:132
  13. Angiotensin II produces nociceptive behavior through spinal AT1 receptor-mediated p38 mitogen-activated protein kinase activation in mice.
    Authors: Nemoto Et al.
    Mol Pain  2013;9:38
  14. High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses.
    Authors: Cruz Et al.
    PLoS Negl Trop Dis  2013;7:e2073
  15. Angiotensin II receptor type 2 activation is required for cutaneous sensory hyperinnervation and hypersensitivity in a rat hind paw model of inflammatory pain.
    Authors: Chakrabarty Et al.
    J Pain  2013;14:1053
  16. Brain-derived neurotrophic factor ameliorates brain stem cardiovascular dysregulation during experimental temporal lobe status epilepticus.
    Authors: Tsai Et al.
    Am J Physiol Heart Circ Physiol  2012;7:e33527
  17. Angiotensin II type 2 receptor-mediated inhibition of NaCl absorption is blunted in thick ascending limbs from Dahl salt-sensitive rats.
    Authors: Hong and Garvin
    Diabetes  2012;60:765
  18. Preferential accumulation and export of high molecular weight FGF-2 by rat cardiac non-myocytes.
    Authors: Santiago Et al.
    Cardiovasc Res  2011;89:139
  19. Angiotensin II signaling up-regulates the immediate early transcription factor ATF3 in the left but not the right atrium.
    Authors: Hasin Et al.
    Basic Res Cardiol  2011;106:175
  20. Identification of noncytotoxic and IL-10-producing CD8+AT2R+ T cell population in response to ischemic heart injury.
    Authors: Curato Et al.
    PLoS One  2010;185:6286
  21. 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.
    Authors: Bourassa Et al.
    Brain Res  2010;1359:98
  22. PPAR- γ inhibits ANG II-induced cell growth via SHIP2 and 4E-BP1.
    Authors: Benkirane Et al.
    Hypertension  2006;290:H390

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