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Pafuramidine

产品编号 T16428 CAS 186953-56-0

别名: DB289

Pafuramidine is an orally bioavailable prodrug of furamidine. It has activity against Pneumocystis pneumonia (IC50 value: 4.5 nM)

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Pafuramidine, CAS 186953-56-0

规格	价格/CNY	货期
2 mg	￥ 1,140	5日内发货
5 mg	￥ 1,930	5日内发货
10 mg	￥ 2,930	5日内发货
1 mL * 10 mM (in DMSO)	￥ 2,120	5日内发货

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其他形式的 Pafuramidine:

Pafuramidine maleate
询价

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Pafuramidine is an orally bioavailable prodrug of furamidine. It has activity against Pneumocystis pneumonia (IC50 value: 4.5 nM)
体外活性	The results of this investigation suggest that DB75 inhibits mitochondrial function. Yeast cells relying upon mitochondrial metabolism for energy production are especially sensitive to DB75 [1].
体内活性	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 [1]. 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 [2]. Despite excellent oral activity against early-stage sleeping sickness, oral administration of DB289 exhibited limited efficacy in mouse models of late-stage disease [3].

别名	DB289
分子量	364.4
分子式	C20H20N4O3
CAS No.	186953-56-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 33.33 mg/mL (91.47 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7442 mL	13.7212 mL	27.4424 mL	68.6059 mL
	5 mM	0.5488 mL	2.7442 mL	5.4885 mL	13.7212 mL
	10 mM	0.2744 mL	1.3721 mL	2.7442 mL	6.8606 mL
	20 mM	0.1372 mL	0.6861 mL	1.3721 mL	3.4303 mL
	50 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3721 mL

计算器

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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. 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. 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. In vitro inhibitory activity against Trypanosoma brucei rhodesiense - BioAssay Summary.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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