Name | PQ 69 |
---|---|
Supplier | Tocris Bioscience |
Catalog | 2768 |
Prices | $225.00, $925.00 |
Sizes | 10 mg, 50 mg |
Function Type | Antagonist |
Cas Number | 910045-32-8 |
Chemical Name | 4-(Butylamino)-2-(3-fluorophenyl)-1,2-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one |
Formula | C20H19FN4O |
Molecular Weight | 350.39 |
Purity | >98 % |
Description | Potent and selective A 1 receptor antagonist/inverse agonist. Exhibits high binding affinity at A 1 receptor (K i values are 0.07 and 0.96 nM for rat and human receptors respectively). Reduces basal [ 35 S]-GTP γ S binding 44.6% (IC 50 = 0.19 nM). Antagonizes the effects of A 1 agonist R-PIA (IC 50 = 18.3 nM) and exhibits competitive antagonism on CCPA -induced tracheal contractions ex vivo . Displays 217- fold selectively over hA 2A receptor and >1000-fold selectivity over hA 3 receptor. |
Supplier Page | Shop |
Gao Y, Lecker S, Post MJ, Hietaranta AJ, Li J, Volk R, Li M, Sato K, Saluja AK, Steer ML, Goldberg AL, Simons M. J Clin Invest. 2000 Aug;106(3):439-48.
Li J, Post M, Volk R, Gao Y, Li M, Metais C, Sato K, Tsai J, Aird W, Rosenberg RD, Hampton TG, Sellke F, Carmeliet P, Simons M. Nat Med. 2000 Jan;6(1):49-55.
Gaczynska M, Osmulski PA, Gao Y, Post MJ, Simons M. Biochemistry. 2003 Jul 29;42(29):8663-70.