Pafuramidine
Cat. No. :YN250614
CAS No. :186953-56-0
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order@ubiochem.com| Product Name: | Pafuramidine |
| CAS NO.: | 186953-56-0 |
| Chemical Name: | |
| Synonyms: | |
| Molecular Weight: | 364.40 |
| Molecular Formula: | C₂₀H₂₀N₄O₃ |
| SMILES: | N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(NOC)=N)C=C3)O2)C=C1)NOC |
| Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Transportation: | Room temperature in continental US; may vary elsewhere. |
| Description: | Pafuramidine (DB289) is an orally bioavailable prodrug of furamidine, which has activity against Pneumocystis pneumonia. DB289 (pafuramidine maleate; 2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) is a prodrug of DB75 (furamidine dihydrochloride; 2,5-bis(4-guanylphenyl)furan dihydrochloride), an aromatic dication related to pentamidine that has demonstrated good efficacy against African trypanosomiasis, Pneumocystis carinii pneumonia, and malaria, but lacks adequate oral availability. 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 . in vivo: 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 . Clinical trial: 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 . |
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