Molecular Formula | C31H32N4O3 |
Molar Mass | 508.61 |
Density | 1.22±0.1 g/cm3(Predicted) |
Boling Point | 775.8±60.0 °C(Predicted) |
Flash Point | 423℃ |
Solubility | H2O: 12mg/mL |
Appearance | powder |
pKa | 2.80±0.20(Predicted) |
Storage Condition | 2-8°C |
In vitro study | PD123319 behaves differently in the two subclasses of receptors used in a variety of different tissues. 125 I--AII specific labeling of the two types of binding in membrane preparation of bovine adrenal glomerulosa cell sites. The first type (DuP-753 sensitive) represents about 85% of the total binding sites and has a high affinity for DUP-753 (92.9 nM for IC 50). PD-123319 does not have any effect on the binding of 125 SUP> I-AII to the standard point. The second type of binding site is more sensitive to PD-123319, the IC 50 is 6.9 nM, and the affinity for DUP-753 is much lower (IC50 value -10 mM). PD123319 behaves differently in the two subclasses of receptors used in a variety of different tissues. |
In vivo study | PD123319 had no effect on self-regulation of cerebral blood flow. Acute AT2 receptor blockade does not affect cerebral autoregulation. Intravenous administration of PD 123319 resulted in a transient dose-dependent increase in MAP in hypertensive rats, with 3 mg/kg of PD123319 resulting in a MAP maintenance of approximately 7.4 minutes. PD123319 had no effect on self-regulation of cerebral blood flow. Acute AT2 receptor blockade does not affect cerebral autoregulation. Intravenous administration of PD 123319 resulted in a transient dose-dependent increase in MAP in hypertensive rats, with 3 mg/kg of PD123319 resulting in a MAP maintenance of approximately 7.4 minutes. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
biological activity | PD123319 is an effective, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. PD123319 is an effective, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. |
in vitro studies | PD123319 are different in two subclasses of receptors used in many different tissues. 125 I--AII specific markers bind two types of bovine adrenal glomerulosa cells to the membrane. The first type (DuP-753 sensitive) represents about 85% of the total binding sites and has a high affinity for DUP-753 (IC 50 is 92.9 nM). PD-123319 will not have any effect on the combination of 125 SUP> I-AII to the standard point. The second type of binding site is more sensitive to PD-123319, IC 50 is 6.9 nM, and the affinity for DUP-753 is much lower (IC50 value is about 10 mM). PD123319 are different in two subclasses of receptors used in many different tissues. |
in vivo studies | PD123319 have no effect on self-regulation of cerebral blood flow. Acute AT2 receptor blockade does not affect cerebral blood flow autoregulation. Intravenous administration of PD 123319 resulted in a transient dose-dependent increase in MAP in hypertensive rats, and a PD123319 of 3 mg/kg resulted in MAP maintenance of about 7.4 minutes. PD123319 has no effect on self-regulation of cerebral blood flow. Acute AT2 receptor blockade does not affect cerebral blood flow autoregulation. Intravenous administration of PD 123319 resulted in a transient dose-dependent increase in MAP in hypertensive rats, and a PD123319 of 3 mg/kg resulted in MAP maintenance of about 7.4 minutes. |
target | TargetValue AT2 receptor 34 nM |
Target | Value |
AT2 receptor | 34 nM |