| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Purity: ≥98%
Pafuramidine, formerly known as DB289, is an orally bioavailable prodrug of furamidine (DB75) which was developed for the treatment of human African trypanosomiasis. Pafuramidine is less toxic than previous diamidines such as pentamidine. To date, human trials suggest that pafuramidine is well tolerated overall and has clinical activity against Pneumocystis pneumonia. DB289 is a promising new antimalarial compound that could become an important component of new antimalarial combinations.
| ln Vivo |
For five or ten days, trypanosome-infected monkeys can be cured by administering pafuradine (1–10 mg/kg) orally [1]. In some Trypanosoma brucei-infected mice, furamidine (2.5–100 mg/kg; oral; for 4–5 days) can be curative [5].
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| Animal Protocol |
Animal/Disease Models: vervet monkey (intravenous (iv) (iv)104 trypanosome infection) [1]
Doses: 1, 3, 10 mg/kg (group 1/2/3); 10 mg/kg (group 4/5) Route of Administration: Oral administration; Group 1/2/3 for 5 days (starting on the 7th day after infection); Group 4 for 10 days (starting on the 14th day after infection); Group 5 for 10 days (starting on the 28th day after infection) ). Post-treatment monitoring continues for 180 days. Experimental Results: All 3 monkeys in the 10 mg/kg group were cured and there was no recurrence during the monitoring period. All three monkeys in Group 4 were parasitic on day 5 of dosing, but only two of the three monkeys were free of blood parasites when monitored 180 days after treatment. All three monkeys in Group 5 were parasitic on day 4 of dosing, but only two of the three monkeys remained free of blood trypanosomatids at the end of 180 days of post-treatment monitoring. Animal/Disease Models: Female NMRI mice (intraperitoneally (ip) (ip) infected with 2 × 104 STIB900 bloodstream form) [5] Doses: 2.5, 5, 25 and 50 mg/kg Route of Administration: p.o.; for 4 days (started on the 4th day postinfection) Experimental Results: Cured all four mice at 25 and 50 mg/kg. Animal/Disease Models: Female NMRI mice (infected intraperitoneally with 2 × 104 GVR35 bloodstream forms)[5] Doses: 25, 50 and 100 mg/kg Route of Administration: p.o.; for 5 days (started on the 21st day postinfection) Experimental Results: Showed good CNS activity in the GVR35 CNS model, with 3/5 mice cured at 100 mg/kg. |
| References |
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| Additional Infomation |
Pafuramidine, a prodrug of furamidine, currently has orphan status for Pneumocystis jiroveci pneumonia.
Drug Indication Investigated for use/treatment in pneumonia, trypanosomiasis, malaria, HIV infection, and infectious and parasitic disease (unspecified). |
| Molecular Formula |
C20H20N4O3
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|---|---|
| Molecular Weight |
364.3978
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| Exact Mass |
364.154
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| CAS # |
186953-56-0
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| Related CAS # |
Pafuramidine maleate;837369-26-3
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| PubChem CID |
5480200
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.25
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| Melting Point |
192.5-193ºC
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| LogP |
4.547
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
477
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CO/N=C(\N)/C1=CC=C(C=C1)C2=CC=C(O2)C3=CC=C(C=C3)/C(=N/OC)/N
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| InChi Key |
UKOQVLAXCBRRGH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H20N4O3/c1-25-23-19(21)15-7-3-13(4-8-15)17-11-12-18(27-17)14-5-9-16(10-6-14)20(22)24-26-2/h3-12H,1-2H3,(H2,21,23)(H2,22,24)
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| Chemical Name |
N'-methoxy-4-[5-[4-[(Z)-N'-methoxycarbamimidoyl]phenyl]furan-2-yl]benzenecarboximidamide
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| Synonyms |
DB289 DB-289 DB 289
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~91.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7442 mL | 13.7212 mL | 27.4424 mL | |
| 5 mM | 0.5488 mL | 2.7442 mL | 5.4885 mL | |
| 10 mM | 0.2744 mL | 1.3721 mL | 2.7442 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00619346 | TERMINATED | Drug: Placebo Drug: pafuramidine maleate |
Healthy | Immtech Pharmaceuticals, Inc | 2007-11 | Phase 1 |
| NCT00803933 | COMPLETED | Drug: DB289 Drug: Pentamidine |
African Trypanosomiasis | Immtech Pharmaceuticals, Inc | 2003-02 | Phase 2 |
| NCT00802594 | COMPLETED | Drug: DB289 | Trypanosomiasis, African | Immtech Pharmaceuticals, Inc | 2001-08 | Phase 2 |
| NCT00408369 | COMPLETED | Drug: DB289 | Prophylactic Activity Against Malaria | Immtech Pharmaceuticals, Inc | 2006-11 | Phase 1 Phase 2 |
| NCT00302341 | TERMINATED | Drug: Pafuramidine maleate (DB289) Drug: Trimethoprim-Sulfamethoxazole (TMP-SMX) |
HIV Infections Pneumocystis Carinii Pneumonia Pneumonia, Interstitial Plasma Cell Pneumonia, Pneumocystis Carinii |
Immtech Pharmaceuticals, Inc | 2006-05 | Phase 3 |
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