Cycloguanil (hydrochloride)
(Synonyms: 环氯胍盐酸盐) 目录号 : GC16333
The active metabolite of proguanil
Cas No.:152-53-4
Sample solution is provided at 25 µL, 10mM.
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Cycloguanil is an inhibitor of dihydrofolate reductase (DHFR)[1].
Dihydrofolate reductase (DHFR) is an enzyme that involved in reducing dihydrofolic acid to tetrahydrofolic acid. DHFR plays a critical role in regulating the amount of tetrahydrofolate in the cell, which are essential for purine and thymidylate synthesis important for cell proliferation and cell growth. DHFR also plays a central role in the synthesis of nucleic acid precursors and salvage of tetrahydrobiopterin from dihydrobiopterin [2].
Cycloguanil is the active metabolite of proguanil produced by the cytochrome P450 (CYP) [3]. Cycloguanil showed activity against P. falciparu. Cycloguanil inhibited the activity of dihydrofolate reductase (DHFR) with the Ki values of 0.3 and 1.5 nM for Plasmodium and human forms, respectively., Cycloguanil prevented the production of tetrahydrofolic acid, an essential coenzyme involved in DNA and RNA synthesis, by blocking DHFR activity.
References:
[1] Foote S J, Galatis D, Cowman A F. Amino acids in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum involved in cycloguanil resistance differ from those involved in pyrimethamine resistance[J]. Proceedings of the National Academy of Sciences, 1990, 87(8): 3014-3017.
[2] Blakley R L. Dihydrofolate reductase[J]. Encyclopedia Of Molecular Medicine, 1984.
[3] Birkett D J, Rees D, Andersson T, et al. In vitro proguanil activation to cycloguanil by human liver microsomes is mediated by CYP3A isoforms as well as by S‐mephenytoin hydroxylase[J]. British journal of clinical pharmacology, 1994, 37(5): 413-420.
| Cas No. | 152-53-4 | SDF | |
| 别名 | 环氯胍盐酸盐 | ||
| 化学名 | 1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamine, monohydrochloride | ||
| Canonical SMILES | ClC1=CC=C(N2C(N)=NC(N)=NC2(C)C)C=C1.Cl | ||
| 分子式 | C11H14ClN5 • HCl | 分子量 | 288.2 |
| 溶解度 | ≤5mg/ml in ethanol;20mg/ml in DMSO;5mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4698 mL | 17.3491 mL | 34.6981 mL |
| 5 mM | 0.694 mL | 3.4698 mL | 6.9396 mL |
| 10 mM | 0.347 mL | 1.7349 mL | 3.4698 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet