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Pafuramidine

Catalog No.GC15249

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Pafuramidine Chemical Structure

Cas No.: 186953-56-0

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5mg
$170.00
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10mg
$275.00
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50mg
$614.00
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100mg
$1,011.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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