氯胍
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- CAS号:
- 500-92-5
- 英文名:
- N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE
- 英文别名:
- bigumal;PROGUANIL;paludrine;Proquanil;Aids008307;Aids-008307;chlorguanide;chloroguanide;ChlorguanideCl;Chlorguanide-D6Cl
- 中文名:
- 氯胍
- 中文别名:
- 氯胍;丙胍杂质;氯胍-D6;氯胍-D6盐酸;N1-(4-氯苯基)-N5-异丙基双胍;N-(4-氯苯基)-N'-(异丙基)-双胍;CHLORGUANIDE (PROGUANIL)
- CBNumber:
- CB7455742
- 分子式:
- C11H16ClN5
- 分子量:
- 253.73
- MOL File:
- 500-92-5.mol
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氯胍化学性质
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熔点:
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129°
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沸点:
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399.65°C (rough estimate)
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密度:
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1.2039 (rough estimate)
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折射率:
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1.6110 (estimate)
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储存条件:
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Store at -20°C, protect from light
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溶解度:
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DMF: 2mg/mL; DMSO: 3mg/mL; DMSO:PBS (pH 7.2) (1:10): 0.09mg/mL; Ethanol: 1mg/mL
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形态:
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A solid
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酸度系数(pKa):
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11.15±0.10(Predicted)
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氯胍性质、用途与生产工艺
Proguanil (chlorguanide, chloroguanide) 是预防性抗疟药。它能抑制疟原虫的二氢叶酸还原酶，阻止嘌呤和嘧啶的合成。
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.
生产方法
由硫氯酸钠与水合肼加成、重排，最后经甲醛在乙醇中缩合而制得。
氯胍
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-B0806 | Proguanil | | 5 mg | 312元 |
| 2024/01/25 | HY-B0806 | 氯胍
Proguanil | 500-92-5 | 10mg | 500元 |
氯胍
生产厂家
全球有 62家供应商
氯胍国内生产厂家
500-92-5, 氯胍 相关搜索:
- C11H16ClN5
- CHLORGUANIDE (PROGUANIL)
- 丙胍杂质
- 氯胍-D6
- N1-(4-氯苯基)-N5-异丙基双胍
- N-(4-氯苯基)-N'-(异丙基)-双胍
- 氯胍-D6盐酸
- 氯胍
- 500-92-5
- N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE
- Pyridoxine Impurity 50 (Pyridoxine Dipalmitate)
- ProguanilQ: What is
Proguanil Q: What is the CAS Number of
Proguanil Q: What is the storage condition of
Proguanil
- N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE USP/EP/BP
- Chlorguanide (Proguanil)
- Proquanil
- Chlorguanide-d6 HCl
- Imidodicarbonimidic diamide, N-(4-chlorophenyl)-N'-(1-methylethyl)-
- Diguanyl (hydrochloride)
- Aids-008307
- Aids008307
- 637-32-1 (Hydrochloride)
- ChlorguanideCl
- Chlorguanide-D6Cl
- Chlorguanide (base and/or unspecified salts)
- 1-(4-chlorophenyl)-5-isopropylbiguanide
- N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE
- PROGUANIL
- paludrine
- chloroguanide
- chlorguanide
- bigumal
- 1-(p-chlorophenyl)-5-isopropylbiguanide
- 1-(p-chlorophenyl)-5-isopropyl-biguanid