Cycloguanil HCl

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Chemical Structure| 152-53-4 同义名 : 环氯胍盐酸盐 ;Cycloguanil (hydrochloride); Cycloguanil hydrochloride; NSC 3074; Chloroguanide Triazine
CAS号 : 152-53-4
货号 : A110956
分子式 : C11H15Cl2N5
纯度 : 99%+
分子量 : 288.18
MDL号 : MFCD00035308
存储条件:

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Cycloguanil HCl, the active metabolite of proguanil, is a dihydrofolate-reductase (DHFR) inhibitor and acts on malaria schizonts in erythrocytes and hepatocytes. A partial cross-resistance between pyrimethamine and cycloguanil that is based on similar amino acid substitutions in dihydrofolate reductase and suggest that two or three mutations, including at least Asn-108, may be necessary for cycloguanil resistance, whereas a single Asn-108 mutation is sufficient for pyrimethamine resistance[1]. The combination of atovaquone and cycloguanil yielded corresponding mean sigmaFICs of 3.70 and 2.11, indicating antagonism. The EC50 and EC90 values for proguanil alone were not influenced by RPMI-1640 medium with low concentrations of paraaminobenzoic acid and folic acid (LPLF culture medium), whereas the EC50 and EC90 values for cycloguanil were more than 10 times lower in LPLF medium than in normal RPMI-1640 medium[2]. Cycloguanil (2.5 micrograms/ml) combined with a noninhibitory concentration of sulfadiazine (25 micrograms/ml) inhibited T. gondii more than cycloguanil alone[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.47mL

0.69mL

0.35mL

17.35mL

3.47mL

1.74mL

34.70mL

6.94mL

3.47mL

参考文献

[1]Basco LK, Ringwald P. Molecular epidemiology of malaria in Yaounde, Cameroon. VI. Sequence variations in the Plasmodium falciparum dihydrofolate reductase-thymidylate synthase gene and in vitro resistance to pyrimethamine and cycloguanil. Am J Trop Med Hyg. 2000 Feb;62(2):271-6

[2]Thapar MM, Gupta S, Spindler C, Wernsdorfer WH, Björkman A. Pharmacodynamic interactions among atovaquone, proguanil and cycloguanil against Plasmodium falciparum in vitro. Trans R Soc Trop Med Hyg. 2003 May-Jun;97(3):331-7

[3]Holfels E, McAuley J, Mack D, Milhous WK, McLeod R. In vitro effects of artemisinin ether, cycloguanil hydrochloride (alone and in combination with sulfadiazine), quinine sulfate, mefloquine, primaquine phosphate, trifluoperazine hydrochloride, and verapamil on Toxoplasma gondii. Antimicrob Agents Chemother. 1994 Jun;38(6):1392-6