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Pafuramidine

Catalog No. T16428 CAS 186953-56-0

Synonyms: 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

Pack Size	Availability	Price/USD
2 mg	5 days	$ 142.00
5 mg	5 days	$ 247.00
10 mg	5 days	$ 377.00
1 mL * 10 mM (in DMSO)	5 days	$ 272.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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

Synonyms	DB289
Molecular Weight	364.4
Formula	C20H20N4O3
CAS No.	186953-56-0

Storage

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

Solubility Information

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

References and Literature

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pafuramidine 186953-56-0 Others DB 289 DB-289 DB289 inhibitor inhibit

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