产品说明

包装

5, 25 mg in glass bottle

生化/生理作用

Highly potent, selective and orally active platelet-activating factor (PAF) receptor antagonist. K_i = 0.6 nM in human platelets.

特点和优势

This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
This compound is featured on the PAF Receptor page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

基本信息

产品性质

安全信息

产品说明

一般描述

An orally available ethynylindole compound that potently inhibits PAF (platelet-activating factor) binding to its receptor in a competitive manner in equilibrium binding studies (K_i = 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.

包装

2 mg in Plastic ampoule
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Curtin, M.L., et al. 1998. J. Med. Chem.41, 74.
Albert, D.H., et al. 1998. J. Pharmacol. Exp. Ther.284, 83.
Albert, D.H., et al. 1997. Eur. J. Pharmacol.325, 69.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息