125030-71-9
- CAS号:125030-71-9
- 英文名:Ro 24-4736
- 中文名:125030-71-9
- CBNumber:CB91355010
- 分子式:C31H20ClN5OS
- 分子量:546.04
- MOL File:125030-71-9.mol
- 熔点 :247-249 °C
- 沸点 :819.6±75.0 °C(Predicted)
- 密度 :1.41±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :2.10±0.40(Predicted)
125030-71-9性质、用途与生产工艺
- 生物活性 Ro 24-4736 是一种长效的选择性血小板活化因子 (PAF) 拮抗剂。
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靶点
PAF
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体外研究
Ro 24-4736 competes with [ 3 H]PAF for its receptor site on dog platelets with an IC 50 of 9.8±1.0 nM and selectively inhibits PAF-induced aggregation of guinea pig, dog and human platelets with concentration dependence.
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体内研究
Ro 24-4736 dose-dependently inhibits in vivo bronchoconstriction (ID50 of 0.006-mg/kg p.o.) and ex vivo platelet aggregation (ID 50 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 14 C-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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