PROGUANIL HYDROCHLORIDE
proguanil hydrochloride
CAS: 637-32-1
Molecular Formula: C11H17Cl2N5
PROGUANIL HYDROCHLORIDE - Names and Identifiers
| Name | proguanil hydrochloride |
| Synonyms | 3359rp diguanyl Proguanil HCL proguanil hydrochloride chlorguanidehydrochloride chloroguanidehydrochloride Chloroguanide hydrochloride chloroguanidinehydrochloride 1-(p-chlorophenyl)-5-isopropylbiguanidehydrochloride N1-(4-Chlorophenyl)-N5-isopropylbiguanide Hydrochloride 1-(p-chlorophenyl)-5-isopropyl-biguanidmonohydrochloride 1-{(1E)-amino[(4-chlorophenyl)amino]methylidene}-2-(1-methylethyl)guanidine hydrochloride |
| CAS | 637-32-1 |
| EINECS | 211-283-7 |
| InChI | InChI=1/C11H16ClN5.ClH/c1-7(2)15-10(13)17-11(14)16-9-5-3-8(12)4-6-9;/h3-7H,1-2H3,(H5,13,14,15,16,17);1H |
PROGUANIL HYDROCHLORIDE - Physico-chemical Properties
| Molecular Formula | C11H17Cl2N5 |
| Molar Mass | 290.19 |
| Melting Point | 249-2510C |
| Boling Point | 402.7°C at 760 mmHg |
| Flash Point | 197.4°C |
| Solubility | acetonitrile: water: ~1mg/mL (60/40) |
| Vapor Presure | 1.07E-06mmHg at 25°C |
| Appearance | solid |
| Storage Condition | 2-8°C |
| In vitro study | 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. |
| In vivo study | 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. |
PROGUANIL HYDROCHLORIDE - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | 3249 |
| WGK Germany | 3 |
| RTECS | DU1750000 |
| HS Code | 2925294500 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
| Toxicity | LD50 orally in rats: 200 mg/kg (Schmidt) |
PROGUANIL HYDROCHLORIDE - Reference Information
| biological activity | Proguanil hydrochloride is an antimalarial prodrug that is metabolized to the active metabolite, cyclic guanosine (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor. |
Last Update：2024-04-10 22:29:15
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Product Name: Proguanil Hydrochloride Visit Supplier Webpage Request for quotationCAS: 637-32-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple Specifications
Product Name: PROGUANIL HYDROCHLORIDE Visit Supplier Webpage Request for quotationCAS: 637-32-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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