吉非罗齐杂质A
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- CAS号:
- 637-32-1
- 英文名:
- Chlorguanide Hydrochloride
- 英文别名:
- m4888;3359rp;diguanyl;Paludrin;sn12,837;Chlorguanid;Chloroquanil;Proguanil HCL;ChlorguanideHCl;PROGUANIL HCL IP/BP
- 中文名:
- 吉非罗齐杂质A
- 中文别名:
- 盐酸氯胍;盐酸丙胍;盐酸氯胍 标准品;盐酸氯胍 USP标准品;N1-(4-氯苯基)-N5-异丙基双胍盐酸盐
- CBNumber:
- CB5488955
- 分子式:
- C11H17Cl2N5
- 分子量:
- 290.19
- MOL File:
- 637-32-1.mol
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吉非罗齐杂质A化学性质
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熔点:
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249-2510C
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储存条件:
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2-8°C
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溶解度:
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acetonitrile: water: ~1mg/mL (60/40)
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形态:
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solid
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吉非罗齐杂质A性质、用途与生产工艺
Proguanil hydrochloride是一种抗疟前药，被代谢为活性代谢物环鸟苷 (HY-12784)。Proguanil hydrochloride是一种二氢叶酸还原酶 (DHFR) 抑制剂。
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.
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- 标准品
- C11H17Cl2N5
- C11H16ClN5HCl
- 盐酸丙胍
- 盐酸氯胍 USP标准品
- 盐酸氯胍 标准品
- N1-(4-氯苯基)-N5-异丙基双胍盐酸盐
- 盐酸氯胍
- 637-32-1
- PROGUANIL HCL IP/BP
- Imidodicarbonimidic diamide, N-(4-chlorophenyl)-N'-(1-methylethyl)-,monohydrochloride
- Proguanil hydrochloride,Proguanil,infection,biguanide,Inhibitor,embryotoxicity,toxicity,inhibit,Parasite,reproductive,antimalarial,Antifolate
- N1-(4-Chlorophenyl)-N5-isopropylbiguanide Hydrochloride
- Proguanil Hydrochloride (1568040)
- Chlorguanide Hydrochloride USP/EP/BP
- 1-(4-Chlorophenyl)-5-(1-methylethyl)biguanide hydrochloride
- Proguanil for system suitability
- Biguanide, 1-(p-chlorophenyl)-5-isopropyl-, monohydrochloride
- PROGUANIL HYDROCHLORIDE
- sn12,837
- palusilhydrochloride
- paludrinehydrochloride
- n-4-chlorophenyl-n(sup5)-isopropyldiguanidehydrochloride
- m4888
- guanatolhydrochloride
- PROGUANIL HYDROCHLORIDE###N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE
- N1-(4-Chlorophenyl)-N5-isopropylbiguanide
- Chlorguanide Hydrochloride3
- Paludrin
- N-(4-Chlorophenyl)-N'-(1-methylethyl)-imidodicarbonimidic Diamide Hydrochloride
- Chlorguanid
- drinupalhydrochloride
- diguanyl
- chloroguanidinehydrochloride
- chloroguanidehydrochloride
- chlorguanidehydrochloride
- 3359rp
- 1-(p-chlorophenyl)-5-isopropyl-biguanidmonohydrochloride
- 1-(p-chlorophenyl)-5-isopropylbiguanidehydrochloride
- ChlorguanideHCl
- Proguanil HCL
- IMidodicarboniMidic diaMide, N-(4-chlorophenyl)-N'-(1-Methylethyl) -, Hydrochloride (1:1)
- Proguanil Hydrochloride (200 mg)
- Chloroquanil