PD123319 Ditrifluoroacetate

PD123319 Ditrifluoroacetate is a potent selective and non-peptide angiotensin AT2 receptor antagonist

Product information

CAS Number: 136676-91-0

Molecular Weight: 736.66

Formula: C35H34F6N4O7

Synonym:

PD-123319 TFA

PD-123319

Related CAS Number:

130663-39-7 (free base)

Chemical Name: (S)-1-(4-(dimethylamino)-3-methylbenzyl)-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid compound with 2,2,2-trifluoroacetic acid (1:2)

Smiles: CN(C)C1=CC=C(CN2C=NC3CN([C@@H](CC2=3)C(O)=O)C(=O)C(C2C=CC=CC=2)C2C=CC=CC=2)C=C1C.OC(=O)C(F)(F)F.OC(=O)C(F)(F)F

InChiKey: GPKQIEZLHVGJQH-ZXVJYWQYSA-N

InChi: InChI=1S/C31H32N4O3.2C2HF3O2/c1-21-16-22(14-15-26(21)33(2)3)18-34-20-32-25-19-35(28(31(37)38)17-27(25)34)30(36)29(23-10-6-4-7-11-23)24-12-8-5-9-13-24;2*3-2(4,5)1(6)7/h4-16,20,28-29H,17-19H2,1-3H3,(H,37,38);2*(H,6,7)/t28-;;/m0../s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 100 mg/mL(196.61 mM). Water: 100 mg/mL(196.61 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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 microM). [2]

In Vivo:

PD 123319 has no effect on cerebral blood flow autoregulation. Acute AT2-receptor blockade does not influence CBF autoregulation. [3]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. [4]

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.

Products are for research use only. Not for human use.