Pafuramidine |
Catalog No.GC15249 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 186953-56-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pafuramidine, an orally bioavailable prodrug of furamidine (DB75) with considerable trypanocidal activity, is an experimental drug for the treatment of pneumocystis pneumonia (PCP). Pafuramidine is well tolerated and has clinical activity against Pneumocystis pneumonia[1].
In vivo: Inmurine models of human African trypanosomiasis, clearance of parasites from the peripheral circulation started 48 h after initiation of treatment with pafuramidineand was complete in all groups 6 days after the first drug dose. Administration of pafuramidine PO or IP at dose rates equal to or greater than 4 mg/kg resulted in 100% cure rates [2]. In the vervet monkey (Chlorocebus [Cercopithecus] aethiops) model of sleeping sickness, pafuramidine (10 mg/kg) completely cured all three monkeys, whereas lower doses of 3 mg/kg and 1 mg/kg cured only one of three and zero of three monkeysin an early-stage infection, respectively. In a late-stage infection, pafuramidine treatment resulted in cure rates of one of three and zero of three monkeys. These data indicated the limited ability of pafuramidine to cross the blood-brain barrier [3].
Clinical trials: Pafuramidinehas reached Phase III clinical trials for the treatment of first stage African sleeping sickness, but development program was halted in 2008 over concerns about liver toxicity and later renal insufficiency in a number of participants in the additional Phase I trial[4].
References:
[1] Chen D, Marsh R, Aberg J A. Pafuramidine for Pneumocystis jiroveci pneumonia in HIV-infected individuals[J]. Expert review of anti-infective therapy, 2007, 5(6): 921-928.
[2] Thuita J K, Karanja S M, Wenzler T, et al. Efficacy of the diamidine DB75 and its prodrug DB289, against murine models of human African trypanosomiasis[J]. Actatropica, 2008, 108(1): 6-10.
[3] Mdachi R E, Thuita J K, Kagira J M, et al. Efficacy of the novel diamidine compound 2, 5-Bis (4-amidinophenyl)-furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma bruceirhodesiense infection in vervet monkeys after oral administration[J]. Antimicrobial agents and chemotherapy, 2009, 53(3): 953-957.
[4] HarrillA H, DeSmet K D, Wolf K K, et al. A mouse diversity panel approach reveals the potential for clinical kidney injury due to DB289 not predicted by classical rodent models[J]. Toxicological Sciences, 2012: kfs238.
Cas No. | 186953-56-0 | SDF | |
Chemical Name | N'-methoxy-4-[5-[4-[(Z)-N'-methoxycarbamimidoyl]phenyl]furan-2-yl]benzenecarboximidamide | ||
Canonical SMILES | CON=C(C1=CC=C(C=C1)C2=CC=C(O2)C3=CC=C(C=C3)C(=NOC)N)N | ||
Formula | C20H20N4O3 | M.Wt | 364.4 |
Solubility | Soluble in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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