名称 | Proguanil hydrochloride |
描述 | Proguanil hydrochloride (Chloroquanil) is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, Proguanil hydrochloride is converted to its active cyclic triazine metabolite, cycloguanil, by a cytochrome P450 dependent reaction. Cycloguanil selectively inhibits the bifunctional dihydrofolate reductase-thymidylate synthase of plasmodium parasite, thereby disrupting deoxythymidylate synthesis and ultimately blocking DNA and protein synthesis in the parasite. |
细胞实验 | Sertoli cells obtained from sixteen to eighteen day-old-rats are cultured and treated with 0.3 μM to 10 μM of proguanil for 5 days after which Sertoli cell viability and nuclei integrity are determined. Also, the genetic expressions of transferrin and Glial cell line-derived neurotrophic factor are assessed. They are for reference only. |
动物实验 | Proguanil is prepared in distilled water.Rats: Groups of ten to twelve-week-old rats are administered proguanil (2.9 mg/kg body weight) daily for 5 days and 6 weeks respectively. Thereafter, body and reproductive organ weights are taken, sperm parameters are analyzed, while the histology of the testis and epididymis are carried out. Also, serum levels of testosterone, luteinizing hormone and follicle stimulating hormone are determined. They are for reference only. |
体外活性 | proguanil appeared to be a substrate of OCT1 and OCT2 with affinities of 8.1 and 9.0 μM, respectively |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 55 mg/mL (189.53 mM)
|
关键字 | Proguanil hydrochloride | Proguanil | infection | Proguanil Hydrochloride | biguanide | Inhibitor | embryotoxicity | toxicity | inhibit | Parasite | reproductive | Chlorguanide Hydrochloride | Paludrine Hydrochloride | antimalarial | Antifolate |
相关产品 | Guanidine hydrochloride | Procaine | Doxycycline | Metronidazole | Hydroxychloroquine | 5-Fluorouracil | Nitazoxanide | Rotenone | Benzyl benzoate | Thymidine | Kojic acid | Kaempferol |
相关库 | 抑制剂库 | 经典已知活性库 | 抗癌上市药物库 | 已知活性化合物库 | 抗衰老化合物库 | FDA 上市药物库 | 抗寄生虫库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |