Fosmidomycin(sodium salt)

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CAS NO:

66508-37-0

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	205.1
Cas No.	66508-37-0
Formula	C₄H₉NO₅P·Na
Synonyms	Antibiotic FR31564,FR31564
Solubility	≤5mg/ml in PBS, pH 7.2
Chemical Name	P-[3-(formylhydroxyamino)propyl]-phosphonic acid, monosodium salt
Canonical SMILES	ON(C([H])=O)CCCP([O-])(O)=O.[Na+]
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Fosmidomycin is a specific inhibitor of 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXP) [1]. Fosmidomycin is an antibiotic originally isolated from bacteria of the genus Streptomyces.

1-deoxy-d-xylulose 5-phosphate reductoisomerase is an enzyme that interconverts DXP and 2-C-methyl-D-erythritol 4-phosphate (MEP) [2].

Fosmidomycin was active against both Gram-negative and Gram-positive bacteria and the human malarial parasite P. falciparum with the IC50 of 290-370 nM[3]. Fosmidomycin inhibited 1-deoxy-d-xylulose 5-phosphate reductoisomerase in an alternative nonmevalonate pathway for terpenoid biosynthesis with IC50 of 8.2 nM [1]. Fosmidomycin has been shown to possess activity against Plasmodium falciparum in vitro and in the mouse model. In patients with acute uncomplicated Plasmodium falciparum malaria, oral administration of 1,200 mg fosmidomycin every 8 h for 7 days was effective in curing uncomplicated Plasmodiumfalciparum malaria in humans [4]. Fosmidomycin was an effective and safe antimalarial drug [4]. The treatment was well tolerated and showed a fast parasite and fever clearance [4].

References:
[1] Kuzuyama T, Shimizu T, Takahashi S, et al. Fosmidomycin, a specific inhibitor of 1-deoxy-D-xylulose 5-phosphate reductoisomerase in the nonmevalonate pathway for terpenoid biosynthesis[J]. Tetrahedron letters, 1998, 39(43): 7913-7916.
[2] Takahashi S, Kuzuyama T, Watanabe H, et al. A 1-deoxy-D-xylulose 5-phosphate reductoisomerase catalyzing the formation of 2-C-methyl-D-erythritol 4-phosphate in an alternative nonmevalonate pathway for terpenoid biosynthesis[J]. Proceedings of the National Academy of Sciences, 1998, 95(17): 9879-9884.
[3] Jomaa H, Wiesner J, Sanderbrand S, et al. Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs[J]. Science, 1999, 285(5433): 1573-1576.
[4] Lell B, Ruangweerayut R, Wiesner J, et al. Fosmidomycin, a novel chemotherapeutic agent for malaria[J]. Antimicrobial agents and chemotherapy, 2003, 47(2): 735-738.

试验操作

细胞实验 [1]：
细胞系	恶性疟原虫菌株
溶解方法	在PBS中的溶解度≤5mg/ml，pH 7.2。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。
反应条件	45nM～370nM
应用	Fosmidomycin对三种不同的恶疟原虫菌株（HB3、A2和Dd2）均有活性，IC50值为45nM～370nM。
动物实验 [1]：
动物模型	啮齿动物温氏疟原虫感染小鼠
剂量	10 mg/kg, 腹腔注射
应用	用大于10 mg / kg的fosmidomycin腹腔注射处理，动物显然不含寄生虫。用5 mg / kg的fosmidomycin处理，寄生虫血症
注意事项	请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。
References: [1]. Jomaa H, Wiesner J, Sanderbrand S, Altincicek B, Weidemeyer C, Hintz M, Türbachova I, Eberl M, Zeidler J, Lichtenthaler HK, Soldati D, Beck E. Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs. Science. 1999 Sep 3;285(5433):1573-6. PubMed PMID: 10477522.