PD 123319 (Synonyms: (S)-(+)-PD 123319)

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PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC₅₀ of 34 nM.

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PD 123319 Chemical Structure

CAS No. : 130663-39-7

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Other In-stock Forms of PD 123319:

PD 123319 ditrifluoroacetate

Other Forms of PD 123319:

PD 123319 ditrifluoroacetate In-stock

9 Publications Citing Use of MCE PD 123319

: PD 123319 purchased from MedChemExpress. Usage Cited in: FASEB J. 2018 Sep;32(9):5051-5062. [Abstract]; HUVECs are starved for 12 h, treated with 10 mg/mL (9.56 μM) of AngII with or without Losartan or PD123319 for 12 h, and are subsequently used for Western blot analysis.

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AT1 Receptor AT2 Receptor

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Description	PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC₅₀ of 34 nM.
IC₅₀ & Target	IC50: 34 nM (AT2 Receptor)^[1]
In Vitro	PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues. ¹²⁵I-AII specifically label 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 microM)^[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. PD 123319 Related Antibodies
Molecular Weight	508.61
Formula	C₃₁H₃₂N₄O₃
CAS No.	130663-39-7
SMILES	O=C([C@@H]1CC2=C(N=CN2CC3=CC=C(N(C)C)C(C)=C3)CN1C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)O
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (277 KB) Handling Instructions (2659 KB)
References	[1]. Blankley CJ, et al. 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. 1991 Nov;34(11):3248-60. [Content Brief] [2]. Boulay G, et al. 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. 1992 Apr;41(4):809-15 [Content Brief] [3]. Estrup TM, et al. No effect of angiotensin II AT(2)-receptor antagonist PD 123319 on cerebral blood flow autoregulation. J Renin Angiotensin Aldosterone Syst. 2001 Sep;2(3):188-92. [Content Brief] [4]. Brillante DG, et al. Effects of intravenous PD 123319 on haemodynamic and arterial stiffness indices in healthy volunteers. J Renin Angiotensin Aldosterone Syst. 2005 Sep;6(2):102-6. [Content Brief]

Animal Administration
^[3]

The lower limit of CBF autoregulation is studied in 16 SHR. Eight animals receive PD 123319, while eight serve as controls. PD 123319 or saline is administered intravenously, and the BP is allowed to stabilise for 10 minutes after the injection and prior to the commencement of the autoregulation study. Haemorrhagic hypotension is subsequently induced by withdrawing blood into a syringe. By this means, BP is reduced stepwise to the lowest obtainable level. Throughout the study, CBF is measured at 10 to 15 mmHg BP intervals.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Blankley CJ, et al. 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. 1991 Nov;34(11):3248-60. [Content Brief]

[2]. Boulay G, et al. 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. 1992 Apr;41(4):809-15 [Content Brief]

[3]. Estrup TM, et al. No effect of angiotensin II AT(2)-receptor antagonist PD 123319 on cerebral blood flow autoregulation. J Renin Angiotensin Aldosterone Syst. 2001 Sep;2(3):188-92. [Content Brief]

[4]. Brillante DG, et al. Effects of intravenous PD 123319 on haemodynamic and arterial stiffness indices in healthy volunteers. J Renin Angiotensin Aldosterone Syst. 2005 Sep;6(2):102-6. [Content Brief]

PD 123319 Related Classifications

Endocrinology Cardiovascular Disease

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD 123319130663-39-7(S)-(+)-PD 123319PD123319PD-123319Angiotensin ReceptorInhibitorinhibitorinhibit

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