66508-37-0

• 常用中文名：膦胺霉素钠盐
• 常用英文名：Fosmidomycin sodium salt
• CAS号：66508-37-0
• 分子式：C₄H₉NNaO₅P
• 分子量：205.08
• 相关类别： 信号通路 抗感染 细菌
• 发布时间：2018-02-14 08:00:00
• 更新时间：2024-01-06 10:39:35
• Fosmidomycin sodium salt 是一种磷酸抗生素和抗疟疾药,对革兰氏阴性菌和革兰氏阳性菌均有活性。

名称

• 中文名: 膦胺霉素
• 英文名: Fosmidomycin Sodium Salt
• 英文别名: Sodium hydrogen [(2S,3R)-3-methyl-2-oxiranyl]phosphonate; sodium,3-[formyl(hydroxy)amino]propyl-hydroxyphosphinate; Phosphonic acid, [(2S,3R)-3-methyloxiranyl]-, sodium salt (1:1)

物化性质

• 沸点: 463.7ºC at 760 mmHg
• 熔点: 189-191ºC
• 分子式: C₄H₉NNaO₅P
• 分子量: 205.08
• 闪点: 234.3ºC
• PSA: 82.70000
• LogP: 0.34710
• 储存条件: -20°C

生物活性

• 描述: Fosmidomycin sodium salt 是一种磷酸抗生素和抗疟疾药,对革兰氏阴性菌和革兰氏阳性菌均有活性。
• 相关类别:
  信号通路 >> 抗感染 >> 细菌
  研究领域 >> 感染
• 体外研究: Fosmidomycin钠盐是一种膦酸抗生素[1] [2],对革兰氏阴性菌和革兰氏阳性菌都有活性[3]。
• 体内研究: 用剂量> 10mg/kg的fosmidomycin腹膜内处理的动物显然没有寄生虫。用5mg/kg的fosmidomycin处理后,寄生虫病<1％。用50或100mg/kg的fosmidomycin口服治疗的动物显然没有寄生虫,并且用20mg/kg药物治疗后寄生虫病<1％。当治疗在4天后终止时观察到复发。在8天的时间内用30mg/kg的fosmidomycin处理的小鼠完全治愈[3]。
• 参考文献:

  [1]. Kojo H, et al. FR-31564, a new phosphonic acid antibiotic: bacterial resistance and membrane permeability. J Antibiot (Tokyo). 1980 Jan;33(1):44-8.

  [2]. Fernandes JF, et al. Fosmidomycin as an antimalarial drug: a meta-analysis of clinical trials. Future Microbiol. 2015;10(8):1375-90.

  [3]. Jomaa H, et al. Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs. Science. 1999 Sep 3;285(5433):1573-6.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : SZ8554000 CHEMICAL NAME : Phosphonic acid, (3-(formylhydroxyamino)propyl)-, monosodium salt CAS REGISTRY NUMBER : 66508-37-0 LAST UPDATED : 199512 DATA ITEMS CITED : 5 MOLECULAR FORMULA : C4-H9-N-O5-P.Na MOLECULAR WEIGHT : 205.10 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >11 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JKXXAF Japanese Kokai Tokyo Koho Patents. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #78-40720 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 8 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JKXXAF Japanese Kokai Tokyo Koho Patents. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #78-40720 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >11 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JKXXAF Japanese Kokai Tokyo Koho Patents. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #78-40720 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 8050 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JKXXAF Japanese Kokai Tokyo Koho Patents. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #78-40720 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : KHFZAN Khimiko-Farmatsevticheskii Zhurnal. Chemical Pharmaceutical Journal. For English translation, see PCJOAU. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.1- 1967- Volume(issue)/page/year: 19(5),668,1985

安全

• 海关编码: 2931900090

合成路线

1417822-59-3 ~39% 66508-37-0

文献：Suresh, Surisetti; Shyamraj, Dharavath; Larhed, Mats Tetrahedron, 2013 , vol. 69, # 3 p. 1183 - 1188

64-18-6 66508-11-0 ~% 66508-37-0

文献：US6680308 B1, ; Page column 15, 16 ;

66508-11-0 100747-87-3 ~95% 66508-37-0

文献：Yazawa, Hisatoyo; Goto, Shunsuke Tetrahedron Letters, 1985 , vol. 26, # 31 p. 3703 - 3706

66508-11-0 2258-42-6 ~68% 66508-37-0

文献：Hemmi; Takeno; Hashimoto; Kamiya Chemical and Pharmaceutical Bulletin, 1982 , vol. 30, # 1 p. 111 - 118

66508-53-0 ~% 66508-37-0

文献：Suresh, Surisetti; Shyamraj, Dharavath; Larhed, Mats Tetrahedron, 2013 , vol. 69, # 3 p. 1183 - 1188

66508-11-0 ~% 66508-37-0

文献：US4206156 A1, ;

上下游产品

上游产品  5
64-18-6 66508-11-0 100747-87-3 2258-42-6
66508-53-0
下游产品  0

海关

海关编码	2931900090
中文概述	2931900090. 其他有机-无机化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:AB(入境货物通关单,出境货物通关单). 最惠国关税:6.5%. 普通关税:30.0%
Summary	2931900090. other organo-inorganic compounds. VAT:17.0%. Tax rebate rate:13.0%. Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward). MFN tariff:6.5%. General tariff:30.0%