氯胍

氯胍

中文名称氯胍
中文同义词氯胍;氯胍-D6盐酸;N-(4-氯苯基)-N'-(异丙基)-双胍;N1-(4-氯苯基)-N5-异丙基双胍;氯胍-D6;丙胍杂质;CHLORGUANIDE (PROGUANIL)
英文名称N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE
英文同义词1-(p-chlorophenyl)-5-isopropyl-biguanid;1-(p-chlorophenyl)-5-isopropylbiguanide;bigumal;chlorguanide;chloroguanide;paludrine;PROGUANIL;N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE
CAS号500-92-5
分子式C11H16ClN5
分子量253.73
EINECS号207-915-6
相关类别
Mol文件500-92-5.mol
结构式氯胍 结构式

氯胍 性质

熔点129°
沸点399.65°C (rough estimate)
密度1.2039 (rough estimate)
折射率1.6110 (estimate)
储存条件Store at -20°C, protect from light
溶解度DMF:2mg/mL;二甲基亚砜:3mg/mL; DMSO:PBS (pH 7.2) (1:10):0.09mg/mL;乙醇:1mg/mL
形态固体
酸度系数(pKa)11.15±0.10(Predicted)

氯胍 用途与合成方法

Proguanil (chlorguanide, chloroguanide) 是预防性抗疟药。它能抑制疟原虫的二氢叶酸还原酶,阻止嘌呤和嘧啶的合成。

Proguanil per se has only weak antimalarial activity in vitro (IC 50 =2.4-19 μM), and its effectiveness depends on the active metabolite Cycloguanil (IC 50 =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-HT 3 receptor responses are reversibly inhibited by Proguanil, the metabolite 4-chlorophenyl-1-biguanide (CPB) and the active metabolite Cycloguanil (CG), with an IC 50 of 1.81, 1.48 and 4.36 μM, respectively.

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.

生产方法 

由硫氯酸钠与水合肼加成、重排,最后经甲醛在乙醇中缩合而制得。

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-B0806Proguanil5 mg312元
2024/01/25HY-B0806氯胍
Proguanil
500-92-510mg500元

氯胍 上下游产品信息

"氯胍"相关产品信息
人参皂甙RG3 丹参酮ⅡA磺酸钠 舍曲林 奥利司他 阿托伐醌 氯喹 恩波环氯胍 1-苯基双胍 吉非罗齐杂质A 氯胍 氯丙胍
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