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Purity: ≥98%
PD 123319 ditrifluoroacetate is a novel, potent, and selective nonpeptide AT2 (angiotensin II) receptor antagonist with IC50 of 34 nM. It causes rat adrenal preparations to lose 125I-labeled angiotensin II from a particular subset of angiotensin II binding sites. To investigate the distinct functions of AT1R and AT2R in models related to vascular research, including hypertension, PD 123319 has been employed. In the microsome binding assay, PD-123319 is found to have an IC50 value of 6.9nM, which inhibits Ang II from binding the bovine zona glomerulosa microsomal preparation.
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| Enzyme Assay |
It has been demonstrated that in a variety of tissues, PD 123319 can distinguish between two subclasses of AII receptors. Two classes of binding sites for AII in a membrane preparation of bovine adrenal glomerulosa cells were specifically labeled by 125I-AII. With a high affinity (IC50 of 92.9 nM) for DuP-753, the first class (DuP-753 sensitive) accounts for about 85% of all AII binding sites. Regarding 125I-AII binding to this site, PD-123319 has no effect. With an IC50 of 6.9 nM for PD-123319 and an IC50 of approximately 10 μM for DuP-753, the second class of binding sites exhibits greater sensitivity to the former.
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| Cell Assay |
Through inhibition of extracellular signal-regulated kinase signaling, PD123319 suppressed osteogenic differentiation of human mesenchymal stem cells.
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| Animal Protocol |
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| References |
| Molecular Formula |
C35H34F6N4O7
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| Molecular Weight |
736.67
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| Exact Mass |
736.23
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| Elemental Analysis |
C, 57.07; H, 4.65; F, 15.47; N, 7.61; O, 15.20
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| CAS # |
136676-91-0
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| Related CAS # |
PD 123319; 130663-39-7
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C=CC(=C1)CN2C=NC3=C2C[C@H](N(C3)C(=O)C(C4=CC=CC=C4)C5=CC=CC=C5)C(=O)O)N(C)C.C(=O)(C(F)(F)F)O.C(=O)(C(F)(F)F)O
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| InChi Key |
GPKQIEZLHVGJQH-ZXVJYWQYSA-N
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| 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
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| Chemical Name |
(6S)-1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-6,7-dihydro-4H-imidazo[4,5-c]pyridine-6-carboxylic acid;2,2,2-trifluoroacetic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (135.75 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3575 mL | 6.7873 mL | 13.5746 mL | |
| 5 mM | 0.2715 mL | 1.3575 mL | 2.7149 mL | |
| 10 mM | 0.1357 mL | 0.6787 mL | 1.3575 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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