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货期:询盘
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MedChemExpress LLC
- CAS号:
125030-71-9
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询盘
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Ro-24-4736
CAS No. : 125030-71-9
MCE 国际站:Ro-24-4736
产品活性:Ro 24-4736 是一种长效的选择性血小板活化因子 (PAF) 拮抗剂。
研究领域:GPCR/G Protein
作用靶点:Platelet-activating Factor Receptor (PAFR)
In Vitro: Ro 24-4736 competes with [3H]PAF for its receptor site on dog platelets with an IC50 of 9.8±1.0 nM and selectively inhibits PAF-induced aggregation of guinea pig, dog and human platelets with concentration dependence.
In Vivo: Ro 24-4736 dose-dependently inhibits in vivo bronchoconstriction (ID50 of 0.006-mg/kg p.o.) and ex vivo platelet aggregation (ID50 of 0.004 mg/kg p.o.) induced by PAF in guinea pigs. Time course studies show complete blockade of PAF-induced platelet aggregation (ex vivo) up to 8 hr after a single p.o. dose of 0.03 mg/kg as well as a long duration of action in vivo (30 hr). The in vivo PAF antagonistic activity is specific because, even at high p.o. doses (up to 10 mg/kg), Ro 24-4736 shows no inhibitory activity toward the bronchoconstrictor effects of leukotriene D4 or histamine. In comparison with other PAF antagonists evaluated in this guinea pig model, Ro 24-4736 is markedly superior in terms of p.o. potency, bioavailability and p.o. duration of action. Studies are also performed with Ro 24-4736 in additional in vivo models. When administered p.o. to sensitized guinea pigs, the drug attenuates inhaled antigen-induced airway hyper-reactivity without effect on bronchoalveolar lavage leukocyte accumulation. Ro 24-4736 is a new platelet activating factor antagonist. The tissue distribution of the 14C-label in male rats following a single intravenous dose of 1.0 mg/kg of 14C-Ro 24-4736 indicats appreciable uptake by the liver, kidney, heart and gastrointestinal tract. Peak plasma and tissue concentrations are seen at 5 minutes after dosing except for the small intestine (4 hrs) and abdominal fat, stomach and large intestine (4 hrs). At 48 hours, only 3.5% of the dose is present in the tissues, and 6.1% in the lumen of the gastrointestinal tracts.
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文献和实验4.3.1 真菌 最近,多数转基因小麦和大麦的田间试验涉及抗真菌研究(表 20. 1 和表 20.2)。 其中一个申请项目来自先正达公司,它们申请在加拿大马的尼托巴种植抗镰刀菌的材料 ( 申请号 06-sbil-295 - wht01-0871-mb007-01) 。其他已报道的研究还包括提高综合抗性[24]、抗网腫黑稿病 (TriZeiia caries) [ 25]、抗白粉病(Blumeria grominis) [26,27 ] 、抗赤霉病 ( gramineamm ) [
CD1-CD8、CD27、CD28、CD38、CD39、CDw60、CD45、CD45RA、CD45RB、CD45RO、CD98、CD99、CD99R、CD100、CDw101 B细胞 CD10、CD19-CD24、CD37、CD40、CD53、CD72-CD75、CDw76、CD77、CD78、CD79a、CD79b、CD80-CD83、CDw84、CD85、CD
) 主要特异性 CD T细胞 CD1-CD8、CD27、CD28、CD38、CD39、CDw60、CD45、CD45RA、CD45RB、CD45RO、CD98、CD99、CD99R、CD100、CDw101 B细胞 CD10、CD19-CD24、CD37、CD40、CD53、CD72-CD75、CDw76、CD77、CD78、CD79a、CD79b、CD80-CD83、CDw84、CD85、CD86 髓系细胞 CDw12、CD13-CDw17、CD32-CD35、CD64、CDw65
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