Pafuramidine, Inhibitor

Pafuramidine

Cat. Num. AAA5755327

• Purity: 98.00%
• Synonyms: Pafuramidine; DB289; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 33.33mg/mL (91.47mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C20H20N4O3
• SMILES: N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(NOC)=N)C=C3)O2)C=C1)NOC
• CAS Number: 186953-56-0
• Target & IC50: Others
• In Vitro: 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].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Pafuramidine, inhibitor

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

References

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