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Pafuramidine

现货
Catalog No.
A3695
furamidine的前药
组合的产品项目
规格价格库存 数量
5mg
¥ 2,325.00
Ship with 10-15 days
10mg
¥ 3,534.00
Ship with 10-15 days
50mg
¥ 8,370.00
Ship with 10-15 days
100mg
¥ 13,020.00
Ship with 10-15 days

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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

StorageStore at -20°C
M.Wt364.4
Cas No.186953-56-0
FormulaC20H20N4O3
SynonymsDB289
SolubilitySoluble in DMSO
Chemical NameN'-methoxy-4-[5-[4-[(Z)-N'-methoxycarbamimidoyl]phenyl]furan-2-yl]benzenecarboximidamide
SDFDownload SDF
Canonical SMILESCON=C(C1=CC=C(C=C1)C2=CC=C(O2)C3=CC=C(C=C3)C(=NOC)N)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

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化学结构

Pafuramidine