CAS NO: | 130663-39-7 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 508.61 |
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Formula | C31H32N4O3 |
CAS No. | 130663-39-7 (free base); |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 100 mg/mL (196.6 mM) |
Water: 100 mg/mL (196.6 mM) | |
Ethanol: 100 mg/mL (196.6 mM) | |
Solubility (In vivo) | Saline: 30 mg/mL |
Synonyms | PD 123319; PD-123319; PD123319 |
In Vitro | In vitro activity: PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues. 125I-AII specifically labeled two classes of binding sites for AII in a membrane preparation of bovine adrenal glomerulosa cells. The first class (DuP-753 sensitive) represents approximately 85% of the total binding sites for AII and possesses a high affinity (IC50 of 92.9 nM) for DuP-753. PD-123319 does not have any effect on 125I-AII binding to this site. The second class of binding sites is more sensitive to PD-123319, with an IC50 of 6.9 nM, and has a much lower affinity for DuP-753 (IC50 around 10 μM). Cell Assay: PD123319 suppressed osteogenic differentiation of human mesenchymal stem cells through inhibition of extracellular signal-regulated kinase signaling. |
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In Vivo | PD 123319 has no effect on cerebral blood flow autoregulation. Acute AT2-receptor blockade does not influence CBF autoregulation. Intravenous administration of PD 123319 to conscious hypertensive rats elicites an immediate dose-dependent increase in MAP that is sustained for approximately 7.4 min with 3 mg/kg PD 123319. |
Animal model | Spontaneously hypertensive rats |
Formulation & Dosage | Dissolved in saline; 0.36 and 1 mg/kg/min; i.v. injection |
References | Mol Pharmacol. 1992 Apr;41(4):809-15; J Renin Angiotensin Aldosterone Syst. 2001 Sep;2(3):188-92. |