Proguanil hydrochloride

CAS No. 637-32-1

Proguanil hydrochloride( Proguanil Hydrochloride | Paludrine | Chloroguanide hydrochloride )

Catalog No. M18939 CAS No. 637-32-1

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 45 In Stock
10MG 54 In Stock
25MG 92 In Stock
50MG 171 In Stock
100MG 306 In Stock
200MG 491 In Stock
500MG 790 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    Proguanil hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    Proguanil Hydrochloride is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.
  • Description
    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.(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 Proguanil, the metabolite 4-chlorophenyl-1-biguanide (CPB) and the active metabolite Cycloguanil (CG), with an IC50 of 1.81, 1.48 and 4.36 μM, respectively.(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.
  • 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 Proguanil, the metabolite 4-chlorophenyl-1-biguanide (CPB) and the active metabolite Cycloguanil (CG), with an IC50 of 1.81, 1.48 and 4.36 μM, respectively.
  • 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.
  • Synonyms
    Proguanil Hydrochloride | Paludrine | Chloroguanide hydrochloride
  • Pathway
    Autophagy
  • Target
    Autophagy
  • Recptor
    dihydrofolate reductase|thymidylate synthase|NADH dehydrogenase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    637-32-1
  • Formula Weight
    290.19
  • Molecular Formula
    C11H17Cl2N5
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    Cl.Clc1ccc(NC(=N)NC(=N)NC(C)C)cc1
  • Chemical Name
    (1E)-1-[amino-(4-chloroanilino)methylidene]-2-propan-2-ylguanidine;hydrochloride

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Gerlinde F. Pl?ger, etal. Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Proguanil Hydrochloride[J]. Journal of Pharmaceutical Sciences, 2018, 163(4):1-21.
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