Proguanil hydrochloride 是一种双胍类抗疟疾剂，在体内代谢形成环胍。它还是一种二氢叶酸还原酶抑制剂。

Proguanil Hydrochloride is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, proguanil 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.

proguanil appeared to be a substrate of OCT1 and OCT2 with affinities of 8.1 and 9.0 μM, respectively

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.

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.

637-32-1

C11H17Cl2N5

290.19

Chlorguanide hydrochloride;Paludrine hydrochloride;盐酸氯胍;Chloroquanil

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years