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    PD123319
    PD123319

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1779
    CAS #: 130663-39-7Purity ≥98%

    Description: PD 123319 [PD-123319; PD123319; (S)-(+)-PD 123319] is a novel, potent, and selective AT2 (angiotensin II) receptor antagonist with anti-hypertensive effects. It inhibits AT2 with an IC50 of 34 nM. It displaces 125I-labeled angiotensin II from a specific subset of angiotensin II binding sites in rat adrenal preparations. PD 123319 has been used to selectively examine the specific roles for AT1R and AT2R in hypertensive and other vascular research-related models. PD-123319 is found to prevent Ang II from binding the bovine zona glomerulosa microsomal preparation with IC50 value of 6.9nM in the binding assay using microsome.

    References: Mol Pharmacol. 1992 Apr;41(4):809-15; J Renin Angiotensin Aldosterone Syst. 2001 Sep;2(3):188-92.

    Related CAS#: 136676-91-0 (ditrifluoroacetate); 130663-39-7 (free base)

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    Molecular Weight (MW)508.61
    FormulaC31H32N4O3
    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 
    SynonymsPD 123319; PD-123319; PD123319


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    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.

    In VivoPD 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 modelSpontaneously hypertensive rats 
    Formulation & DosageDissolved 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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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