PD 123319 ditrifluoroacetate

Pricing Availability Delivery Time Qty
Cat.No. 1361 - PD 123319 ditrifluoroacetate | C31H32N4O3.2CF3CO2H | CAS No. 130663-39-7
Description: Potent, selective non-peptide AT2 antagonist
Chemical Name: 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)
Datasheet
Citations (19)
Literature

Biological Activity

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
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 130663-39-7
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 51.06 100

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 solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: PD 123319 ditrifluoroacetate, supplier, Potent, selective, non-peptide, AT2, antagonists, Receptors, Angiotensin, PD123319, ditrifluoroacetate, Angiotensin, AT2, Receptors, Angiotensin, AT2, Receptors, Tocris Bioscience

19 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

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

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

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

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

Gu et al (2016) Angiotensin-converting enzyme 2 inhibits lung injury induced by respiratory syncytial virus. J Immunol 6 19840 PMID: 26813885

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

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

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

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


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