W1770
WR99210
别名:
1,6-二氢-6,6-二甲基-1-[3-（2,4,5-三氯苯氧基）丙氧基]-1,3,5-三嗪-2,4-二胺
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关于此项目
经验公式（希尔记法）:
C14H18Cl3N5O2
化学文摘社编号:
分子量:
394.68
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352202
MDL number:
InChI
1S/C14H18Cl3N5O2/c1-14(2)21-12(18)20-13(19)22(14)24-5-3-4-23-11-7-9(16)8(15)6-10(11)17/h6-7H,3-5H2,1-2H3,(H4,18,19,20,21)
SMILES string
CC1(C)N=C(N)N=C(N)N1OCCCOc2cc(Cl)c(Cl)cc2Cl
InChI key
MJZJYWCQPMNPRM-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to off-white
solubility
DMSO: 0.2 mg/mL, clear (warmed)
storage temp.
2-8°C
Biochem/physiol Actions
WR99210 是恶性疟原虫二氢叶酸还原酶 (DHFR) 的强效抑制剂，DHFR 是主要的疟疾药物靶点。它对野生型、双突变型和四突变型二氢叶酸还原酶具有亚纳摩尔级的效价。
二氢叶酸还原酶 (DHFR) 抑制剂。
wgk
WGK 3
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
Manoj T Duraisingh et al.
International journal for parasitology, 32(1), 81-89 (2002-02-14)
The genome sequence of Plasmodium falciparum, the causative agent of the most severe form of malaria in humans, rapidly approaches completion, but our ability to genetically manipulate this organism remains limited. Chromosomal integration has only been achieved following the prolonged
Chris J Janse et al.
Nature protocols, 1(1), 346-356 (2007-04-05)
This protocol describes a method of genetic transformation for the rodent malaria parasite Plasmodium berghei with a high transfection efficiency of 10(-3)-10(-4). It provides methods for: (i) in vitro cultivation and purification of the schizont stage;(ii) transfection of DNA constructs
T F de Koning-Ward et al.
Molecular and biochemical parasitology, 117(2), 155-160 (2001-10-19)
The limited number of selectable markers available for malaria transfection has hindered extensive manipulation of the Plasmodium falciparum genome and subsequently thorough genetic analysis of this organism. In this paper, we demonstrate that P. falciparum is highly sensitive to the
E G Hankins et al.
Molecular and biochemical parasitology, 117(1), 91-102 (2001-09-12)
We have expressed dhfr alleles of Plasmodium falciparum in the budding yeast, Saccharomyces cerevisiae, and used this yeast model to identify single amino acid substitutions that confer high level pyrimethamine resistance on the background of the triple mutant dhfr (I51+R59+N108).
Reinaldo Teixeira Delfino et al.
Biophysical chemistry, 98(3), 287-300 (2002-07-20)
The development of drug resistance is reducing the efficiency of antifolates as antimalarials. This phenomenon has been linked to the occurrence of mutations in the parasite's dihydrofolate reductase (DHFR). In this way, the resistance to pyrimethamine and cycloguanil, two potent
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