氯胍
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 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.
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。
氯胍 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-04-30 | HY-B0806 | 5 mg | 312 | ||
| 2024-04-30 | HY-B0806 | 氯胍 | 500-92-5 | 10mg | 500 |
