A81988

A81988 is a potent, competitive, non-peptidic antagonist of angiotensin AT1 receptors.

Product information

CAS Number: 141887-34-5

Molecular Weight: 414.46

Formula: C23H22N6O2

Chemical Name: 2-[propyl({[2'-(2H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl})amino]pyridine-3-carboxylic acid

Smiles: CCCN(CC1C=CC(=CC=1)C1=CC=CC=C1C1=NNN=N1)C1=NC=CC=C1C(O)=O

InChiKey: DLMNZGAILMQDHA-UHFFFAOYSA-N

InChi: InChI=1S/C23H22N6O2/c1-2-14-29(22-20(23(30)31)8-5-13-24-22)15-16-9-11-17(12-10-16)18-6-3-4-7-19(18)21-25-27-28-26-21/h3-13H,2,14-15H2,1H3,(H,30,31)(H,25,26,27,28)

Technical Data

Appearance: Solid Power

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

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:

A81988 (A-81988) is labeled with tritium to high specific activity (16 Ci/mmol) and radioligand binding assays performed in rat liver membranes. [3H]A81988 binds with high affinity (KD=0.57 nM) and the KD determined from kinetics assays is similar. Non-specific binding (defined with 1 μM angiotensin-II) is very low (< 6% at the KD). The binding of [3H]A81988 is competitive and exhibits appropriate pharmacological specificity for compounds acting at angiotensin AT1 receptors.

In Vivo:

To verify this hypothesis, B2-/- or wild-type mice (B2+/+) are administered a nonpeptide antagonist of Ang II type 1 (AT1) receptors (A81988) from conception through 180 days of age. Untreated B2+/+ and B2-/- served as controls. Blood pressure (BP) and heart rate are monitored with the use of tail-cuff plethysmography at regular intervals. Ventricular weights, diameters, wall thickness, chamber volume, and myocardial fibrosis are measured at 40 and 180 days. No differences are observed in BP, heart rate, and cardiac weight and dimensions between treated and untreated B2+/+. The BP of AT1 antagonist-treated B2-/- is reduced until 70 days; then, it increases to the levels found in untreated B2-/-. AT1 receptor blockade results in a reduction in left ventricular mass, chamber volume, and wall thickness and abrogated myocardial fibrosis in B2-/-. A81988 (A-81988) decreases the BP of Bk2r-/- either in normosodic conditions or after sodium deprivation, whereas in Bk2r+/+ it produces a modest decrease under hyposodic conditions only.

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