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PAF Receptor Antagonist, ABT-491
1-(N,N-Dimethylcarbamoyl)-4-ethynyl-3-(3-fluoro-4-((1H-2-methylimidazo[4,5-c]pyridin-1-yl)methyl)benzoyl)-indole, HCl
An orally available ethynylindole compound that potently inhibits PAF (platelet-activating factor) binding to its receptor in a competitive manner in equilibrium binding studies (Ki = 0.6 or 3.8 nM, respectively, using intact human platelets or isolated rabbit platelet membrane; [PAF] = 0.6 nM), while a non-competitive inhibition is observed if the membrane-bound receptors are pre-incubated with the antagonist prior to the addition of PAF, presumably due to a slower antagonist dissociation rate. Shown to effectively antagonize PAF-induced platelet and neutrophil responses at submicromolar concentrations in vitro and exhibit in vivo efficacy in alleviating PAF-mediated inflammatory and pathological processes in various animals, including guinea pigs, mice, and rats, via either i.v. or p.o.. Reported to display high specificity toward PAF receptor as evaluated in binding assays employing a wide variety of receptors and ion channels.
产品信息
Form Off-white solid
Molar mass 516.
Protect from Light 是的
Hygrocopic 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility H2O
Chemical formula C28H22FN5O2 • HCl
CAS number 189689-94-9
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |