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/ Pyrimethamine

乙嘧啶 /Pyrimethamine {[allProObj[0].p_purity_real_show]}

货号：A195764 同义名： 乙胺嘧啶 / Pirimecidan;Pirimetamin

Pyrimethamine inhibits multidrug and toxin extrusion (MATE) transporter potently, it also inhibits dihydrofolate reductase (DHFR), used for protozoal infections and interferes with tetrahydrofolic acid synthesis from folic acid. Pyrimethamine inhibits adult polycystic kidney disease by modulating STAT signaling pathways.

Pyrimethamine 化学结构 CAS号：58-14-0
Pyrimethamine 化学结构
CAS号：58-14-0
Pyrimethamine 3D分子结构
CAS号：58-14-0
Pyrimethamine 化学结构 CAS号：58-14-0
Pyrimethamine 3D分子结构 CAS号：58-14-0
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Pyrimethamine 纯度/质量文件 产品仅供科研

货号：A195764 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 DHFR ↓ 其他靶点 纯度
Pralatrexate ✔ 99%+
Pemetrexed disodium ++++

DHFR, Ki: 7.2 nM

 		99.9%
Pyrimethamine ++

DHFR, IC50: 15.4 nM

 		98% HPLC
Pemetrexed ++++

DHFR , Ki: 7.2 nM

 		99+%
Methotrexate +

hDHFR, IC50: 24 nM

 		99% (contain ~10%water)
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 STAT1 ↓ STAT3 ↓ STAT5 ↓ 其他靶点 纯度
Nifuroxazide ✔ 98%
Fludarabine ✔ 98%
Artesunate ✔ 98%
BP-1-102 +++

STAT3, Kd: 504 nM

 		99%+
Niclosamide ++

STAT3, IC50: 0.7 μM

 		98%
Napabucasin ✔ 98%
Cryptotanshinone ++

STAT3, IC50: 4.6 μM

 		98%
Stattic +

STAT3, IC50: 5.1 μM

 		98%
NSC 74859 +

STAT3, IC50: 86 μM

 		99%+
Ochromycinone ✔ 98%
HO-3867 ✔ 97%
C188-9 ++++

STAT3, Kd: 4.7 nM

 		99%+
HJC0152 ✔ 98%
SH5-07 ✔ 97%
SH-4-54 ++++

STAT3, Kd: 300 nM

 		+++

STAT5, Kd: 464 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Pyrimethamine 生物活性

靶点

  • DHFR

    DHFR, IC50:15.4 nM
描述 Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR). Based on susceptibility levels, 73 and 68 of 96 fresh clinical isolates were susceptible to pyrimethamine (mean IC50 15.4 nM) and cycloguanil (mean IC50 11.1 nM), respectively. A highly significant positive correlation was found between pyrimethamine and cycloguanil, indicating in vitro cross-resistance between these antifolates[3]. Additionally, pyrimethamine failed to repress levels of SOD1 protein in HeLa cells or homogenates of liver, spinal cord and brain of wild-type mice[4]. The combinations of fluconazole plus sulfadiazine and pyrimethamine or fluconazole plus pyrimethamine were remarkably effective against T. gondii in vivo[5]. Sulfadoxine/pyrimethamine is well tolerated as treatment and when used as intermittent preventive treatment in pregnant African women[6].

Pyrimethamine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00164710 Malaria, Falciparum Phase 4 Completed - Malawi ... 展开 >> Kawale Health Center Lilongwe, Lilongwe District, Malawi Machinga District Hospital Liwonde, Machinga District, Malawi Matiki Health Center Dwangwa, Nkhotakota District, Malawi 收起 <<
NCT00711906 Malaria in Pregnancy Phase 3 Terminated(Malaria prev. fell ... 展开 >>in the study area, so we cannot evaluate the primary endpoint) 收起 << - Zambia ... 展开 >> Choma hospital Choma, Zambia Shampande Clinic Shampande, Zambia 收起 <<
NCT01084213 Malaria Pregn... 展开 >>ancy Anaemia 收起 << Phase 4 Completed - Burkina Faso ... 展开 >> Université de Ouagadougou Ouagadougou, Burkina Faso Gambia Medical Research Council Laboratories Basse, Gambia Ghana Navrongo Health Research Centre Navrongo, Ghana Mali Medical Research and Training Centre Bamako, Mali 收起 <<

Pyrimethamine 参考文献

[1]Maegawa GH, Tropak M, et al. Pyrimethamine as a potential pharmacological chaperone for late-onset forms of GM2 gangliosidosis. J Biol Chem. 2007 Mar 23;282(12):9150-61.

[2]Akao M, Teshima Y, Marban E. Antiapoptotic effect of nicorandil mediated by mitochondrial atp-sensitive potassium channels in cultured cardiac myocytes. J Am Coll Cardiol. 2002 Aug 21;40(4):803-10.

[3]Basco LK, Ramiliarisoa O, Le Bras J. In vitro activity of pyrimethamine, cycloguanil, and other antimalarial drugs against African isolates and clones of Plasmodium falciparum. Am J Trop Med Hyg. 1994 Feb;50(2):193-9

[4]Wright PD, Huang M, Weiss A, Matthews J, Wightman N, Glicksman M, Brown RH Jr. Screening for inhibitors of the SOD1 gene promoter: pyrimethamine does not reduce SOD1 levels in cell and animal models. Neurosci Lett. 2010 Oct 4;482(3):188-92

[5]Martins-Duarte ÉS, de Souza W, Vommaro RC. Toxoplasma gondii: the effect of fluconazole combined with sulfadiazine and pyrimethamine against acute toxoplasmosis in murine model. Exp Parasitol. 2013 Mar;133(3):294-9

[6]Taylor WR, White NJ. Antimalarial drug toxicity: a review. Drug Saf. 2004;27(1):25-61

Pyrimethamine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.02mL

0.80mL

0.40mL

20.10mL

4.02mL

2.01mL

40.21mL

8.04mL

4.02mL

Pyrimethamine 技术信息

CAS号58-14-0
分子式C12H13ClN4
分子量 248.71
别名 乙胺嘧啶 ;Pirimecidan;Pirimetamin;NSC 3061;Khloridin;Daraprim®;Darapram;RP 4753
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 18 mg/mL(72.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Pyrimethamine | Pirimecidan;Pirimetamin;NSC 3061;Khloridin;Daraprim®;Darapram;RP 4753 | 乙胺嘧啶 | Insecticide | Insect Repellent | STAT | Antiparasitic | DHFR | AmBeed-信号通路专用抑制剂 | Pyrimethamine 纯度/质量文件 | Pyrimethamine 亚型比较 | Pyrimethamine 生物活性 | Pyrimethamine 临床数据 | Pyrimethamine 参考文献 | Pyrimethamine 实验方案 | Pyrimethamine 技术信息

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