| 产品描述： | Pafuramidine is an orally bioavailable prodrug of furamidine. It has activity against Pneumocystis pneumonia (IC50 value: 4.5 nM) |
| 靶点： |
Others |
| 体内研究： |
DB289, a novel orally active prodrug of DB75, is undergoing phase IIb clinical trials for early-stage human African trypanosomiasis, Pneumocystis jiroveci carinii pneumonia, and malaria. Clearance of DB289 approximated the liver plasma flow and its large volume of distribution was consistent with extensive tissue binding. Plasma protein binding of DB289 was 97 to 99% in four animal species and humans, but that of DB75 was noticeably less and more species- and concentration-dependent. Despite excellent oral activity against early-stage sleeping sickness, oral administration of DB289 exhibited limited efficacy in mouse models of late-stage disease |
| 参考文献： |
1. Lanteri CA, Trumpower BL, Tidwell RR, DB75, a novel trypanocidal agent, disrupts mitochondrial function in Saccharomyces cerevisiae. Antimicrob Agents Chemother. 2004 Oct;48(10):3968-74. 2. In vitro inhibitory activity against Trypanosoma brucei rhodesiense - BioAssay Summary. 3. Sturk LM, Brock JL, Bagnell CR, Distribution and quantitation of the anti-trypanosomal diamidine 2,5-bis(4-amidinophenyl)furan (DB75) and its N-methoxy prodrug DB289 in murine brain tissue. Acta Trop. 2004 Jul;91(2):131-43. 4. Midgley I, Fitzpatrick K, Taylor LM, Pharmacokinetics and metabolism of the prodrug DB289 (2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) in rat and monkey and its conversion to the antiprotozoal/antifungal drug DB75 (2,5-bis(4-guanylphenyl)furan dihydrochloride). Drug Metab Dispos. 2007 Jun;35(6):955-67. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.744 ml |
13.721 ml |
27.442 ml |
| 5 mM |
0.549 ml |
2.744 ml |
5.488 ml |
| 10 mM |
0.274 ml |
1.372 ml |
2.744 ml |
| 50 mM |
0.055 ml |
0.274 ml |
0.549 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京