[CAS NO. 130663-39-7] PD123319

Name: PD123319
Brand: Arctom Scientific
SKU: AS352194

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PRODUCTS SPECIFICATIONS [130663-39-7]

Distributor

Catalog

AS352194

Brand

Arctom Scientific

CAS

130663-39-7

DESCRIPTION [130663-39-7]

Overview

MDL	MFCD00896427
Molecular Weight	508.61
Molecular Formula	C31H32N4O3
SMILES	C(N1C2=C(CN(C(C(C3=CC=CC=C3)C4=CC=CC=C4)=O)[C@H](C(O)=O)C2)N=C1)C5=CC(C)=C(N(C)C)C=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

PD 123319 is a potent, selective antagonist with of 34 nM.

Targets

AT2 receptor ^[1]

34 nM

In vitro

PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues. I-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 I-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).

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.

References

[1] Blankley CJ, et al. J Med Chem, 1991, 34(11), 3248-3260.
[2] Boulay G, et al. Mol Pharmacol, 1992, 41(4), 809-815.
[3] Estrup TM, et al. J Renin Angiotensin Aldosterone Syst, 2001, 2(3), 188-192.
[4] Tamura M, et al. J Hypertens, 2000, 18(9), 1239-1246.

Synonyms

1H-Imidazo[4,5-c]pyridine-6-carboxylic acid, 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-, (6S)-

1H-Imidazo[4,5-c]pyridine-6-carboxylic acid, 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-, (S)-

1H-Imidazo[4,5-c]pyridine-6-carboxylic acid, 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-, (6S)-

(6S)-1-[[4-(Dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid

PD 123319

(S)-(+)-PD 123319