Pafuramidine
Based on 1 publication(s) in Google Scholar
Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.28%
- No. CAS: 186953-56-0
- Fòrmula: C20H20N4O3
- Peso molecular:364.40
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Anti-COVID-19 Compound Library
HY-L052
-
Orally Active Compound Library
HY-L061
-
Antibiotics Library
HY-L067
-
Antiparasitic Compound library
HY-L082
-
Human Metabolite Library
HY-L123
-
Heterocyclic Compound Library
HY-L138
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Anti-Infection Compound Library
HY-L002
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
Publications Citing Use of MedChemExpress (MCE) Pafuramidine
MoreVer todos los productos específicos de isoformas Parasite
MoreVer todos los productos específicos de isoformas Antibiotic
More
Actividad biológica
|
Trypanosoma |
Plasmodium falciparum sporozoites |
Pafuramidine (2.5-100 mg/kg; p.o.; for 4 or 5 days) cures some Trypanosoma brucei-infected mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Vervet monkeys (infected by intravenous injection of 104 trypanosomes)[1]
-
Dosage:1, 3, and 10 mg/kg (group 1/2/3); 10 mg/kg (group 4/5)
-
Administration:p.o.; 5 consecutive days for group 1/2/3 (started on the 7th day postinfection); 10 days for group 4 (started on the 14th day postinfection); 10 days for group 5 (started on the 28th day postinfection). Post-treatment monitoring was maintained for a period of 180 days.
-
Result:Cured all three monkeys in group 3 at 10 mg/kg, and did not recur during the monitoring period.
All three monkeys in group 4 became aparasitemic by day 5 of dosing, but only two of three monkeys remained free of blood parasites until 180 days post-treatment monitoring.
All three monkeys in group 5 became aparasitemic by day 4 of dosing, but only two of three of monkeys remained free of blood trypanosomes by the end of the 180 days of post-treatment monitoring.
-
Animal Model:Female NMRI mice (infected intraperitoneally with 2 × 104 STIB900 bloodstream forms)[5]
-
Dosage:2.5, 5, 25 and 50 mg/kg
-
Administration:p.o.; for 4 days (started on the 4th day postinfection)
-
Result:Cured all four mice at 25 and 50 mg/kg.
-
Animal Model:Female NMRI mice (infected intraperitoneally with 2 × 104 GVR35 bloodstream forms)[5]
-
Dosage:25, 50 and 100 mg/kg
-
Administration:p.o.; for 5 days (started on the 21st day postinfection)
-
Result:Showed good CNS activity in the GVR35 CNS model, with 3/5 mice cured at 100 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 186953-56-0
-
Appearance Solid
-
Peso molecular 364.40
-
Fòrmula C20H20N4O3
-
Color Off-white to light yellow
-
SMILES
N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(NOC)=N)C=C3)O2)C=C1)NOC
-
Synonyms
DB289
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Molecules
Involvement of CYP4F2 in the Metabolism of a Novel Monophosphate Ester Prodrug of Gemcitabine and Its Interaction Potential In Vitro. [Abstract]2018 May 16;23(5):1195. PMID: 29772747
Solvente y solubilidad
DMSO : 33.33 mg/mL (91.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (277 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Mdachi RE, et al. Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration. Antimicrob Agents Chemother. 2009 Mar;53(3):953-7. [Content Brief]
[2]. Pohlig G, et al. Efficacy and Safety of Pafuramidine versus Pentamidine Maleate for Treatment of First Stage Sleeping Sickness in a Randomized, Comparator-Controlled, International Phase 3 Clinical Trial. PLoS Negl Trop Dis. 2016 Feb 16;10(2):e0004363. [Content Brief]
[3]. Chen D, et al. Pafuramidine for Pneumocystis jiroveci pneumonia in HIV-infected individuals. Expert Rev Anti Infect Ther. 2007 Dec;5(6):921-8. [Content Brief]
[4]. Purfield AE, et al. Interactions of DB75, a novel antimalarial agent, with other antimalarial drugs in vitro. Antimicrob Agents Chemother. 2008 Jun;52(6):2253-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 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 | |
| 15 mM | 0.1829 mL | 0.9147 mL | 1.8295 mL | 4.5737 mL | |
| 20 mM | 0.1372 mL | 0.6861 mL | 1.3721 mL | 3.4303 mL | |
| 25 mM | 0.1098 mL | 0.5488 mL | 1.0977 mL | 2.7442 mL | |
| 30 mM | 0.0915 mL | 0.4574 mL | 0.9147 mL | 2.2869 mL | |
| 40 mM | 0.0686 mL | 0.3430 mL | 0.6861 mL | 1.7151 mL | |
| 50 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.3721 mL | |
| 60 mM | 0.0457 mL | 0.2287 mL | 0.4574 mL | 1.1434 mL | |
| 80 mM | 0.0343 mL | 0.1715 mL | 0.3430 mL | 0.8576 mL |
Pafuramidine Related Classifications
HY-14932 Related Classifications
Powered by Bioz