Proguanil|500-92-5|(氯胍)-陌孚医药/Medlife

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Proguanil (Synonyms: 氯胍)

目录号: PL05423 纯度: ≥99%

CAS No. :500-92-5

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中文名称	Proguanil
中文别名	Chlorguanide(氯胍);Chlorguanide-D6盐酸;氯苯胍;氯胍;氯胍标准品;N-(4-氯苯基)-N'-(异丙基)-双胍
英文名称	Proguanil
英文别名	Imidodicarbonimidicdiamide, N-(4-chlorophenyl)-N'-(1-methylethyl)-;Chlorguanide;N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE;Proguanil;PROGUANIL IMPURITY D 1,5-BIS(1-METHYLETHYL)BIGUANIDE, EP STANDARD;bigumal;ChlorguanideCl;Chlorguanide-D6Cl;chloroguanide;paludrine;Paludrin;Chlorguanid;Proguanilum;Proguanile [DCIT];1-(p-Chlorophenyl)-5-isopropylbiguanide;Proguanil [INN:BAN];Proguanilum [INN-Latin];N1-p-Chlorophenyl-N5-isopropylbiguanide;1-Isopropyl-5-(4-chlorophenyl)biguanide;C11H16ClN5;Imidodicarbonimidic diamide, N-(4-chlorophenyl)-N'-(1-methylethyl)-;S61K3P7B2V;BIGUANIDE, 1-(p-CHLOROPHENYL)-5-ISOPROPYL-;Chloriguane;Proguanile;N-(4-chlo
Cas No.	500-92-5
分子式	C₁₁H₁₆ClN₅
分子量	253.73
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Proguanil 是一种抗疟前药，被代谢为活性代谢物环鸟苷 (HY-12784)。Proguanil 是一种二氢叶酸还原酶 (DHFR) 抑制剂。

生物活性

Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.

性状

Solid

体外研究(In Vitro)

Proguanil per se has only weak antimalarial activity in vitro (IC50=2.4-19 μM), and its effectiveness depends on the active metabolite Cycloguanil (IC50=0.5-2.5 nM). The Cycloguanil is a dihydrofolate reductase (DHFR) inhibitor. The combination of Atovaquone and Proguanil is synergistic in vitro . Both drugs also have activity against gametocytes and pre-erythrocytic (hepatic) stages of malaria parasites.
Proguanil acts as a biguanide rather than as its metabolite Cycloguanil (a parasite dihydrofolate reductase [DHFR] inhibitor) to enhance the Atovaquone effect. Proguanil-mediated enhancement is specific for Atovaquone, since the effects of other mitochondrial electron transport inhibitors, such as Myxothiazole and Antimycin, are not altered by inclusion of Proguanil.
5-HT3 receptor responses are reversibly inhibited by Pr

体内研究(In Vivo)

Proguanil (p.o.; 2.9 mg/kg body weight; daily for 5 days and 6 weeks respectively) shows mild degenerative changes for five days, while shows severe degenerative changes for six weeks in wistar strain albino rats.
Serum testosterone level is significantly decreased for proguanil treatment rats.
Administration of Malarone (atovaquone and proguanil) to experimentally B. gibsoni infected two dogs in chronic stage and three dogs in acute stage results in decrease in parasitemia, and clinical improvements are observed. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Pudney M, et al. Atovaquone and proguanil hydrochloride: a review of nonclinical studies. J Travel Med. 1999 May;6 Suppl 1:S8-12.
[2]. Srivastava IK, et al. A mechanism for the synergistic antimalarial action of atovaquone and proguanil. Antimicrob Agents Chemother. 1999 Jun;43(6):1334-9.
[3]. Lochner M, et al.

溶解度数据	In Vitro: DMSO : ≥ 130 mg/mL (512.36 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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