125030-71-9
125030-71-9 structure
- Name: Ro-24-4736
- Chemical Name: 5-(3-(4-(2-Chlorophenyl)-9-methyl-6H-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propynyl)phenanthridin-6(5H)-one
- CAS Number: 125030-71-9
- Molecular Formula: C31H20ClN5OS
- Molecular Weight: 546.04100
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2017-06-14 20:52:22
- Modify Date: 2024-01-09 16:37:29
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Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action.
| Name | 5-(3-(4-(2-Chlorophenyl)-9-methyl-6H-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propynyl)phenanthridin-6(5H)-one |
|---|---|
| Synonyms |
5-{3-[4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a] [1,4]diazepin-2-yl]-2-propynyl}phenanthridin-6(5H)-one
Ro-24-4736 6(5H)-Phenanthridinone,5-(3-(4-(2-chlorophenyl)-9-methyl-6H-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propynyl) |
| Description | Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action. |
|---|---|
| Related Catalog | |
| Target |
PAF[1] |
| 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[1]. |
| 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[1]. 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[2]. |
| References |
| Density | 1.41g/cm3 |
|---|---|
| Boiling Point | 819.6ºC at 760mmHg |
| Molecular Formula | C31H20ClN5OS |
| Molecular Weight | 546.04100 |
| Flash Point | 449.5ºC |
| Exact Mass | 545.10800 |
| PSA | 93.31000 |
| LogP | 5.59700 |
| Vapour Pressure | 5.81E-27mmHg at 25°C |
| Index of Refraction | 1.749 |
| Storage condition | 2-8℃ |