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• 试剂商城
• 直接询价

分类

• {SNA} A to C, Alanine hydroxymethyltransferase, D-, Biochemicals and Reagents, Cell Biology, Cell Signaling and Neuroscience, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, Peptides and Proteins, Peptides for Cell Biology
• {SNA} A to C, Alanine hydroxymethyltransferase, D-, Biochemicals and Reagents, Cell Signaling and Neuroscience, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, Peptides and Proteins, Peptides for Cell Biology, 细胞生物学
• {SNA} A to C, Alanine hydroxymethyltransferase, D-, Biochemicals and Reagents, Enzyme Inhibitors,
• {SNA} A to C,

产品应用

• An irreversible inhibitor of 3-ketodihydrosphingosine synthetase

相关文献及参考

• 1. Cinati, J. Jr., et al., Cytotoxicity of L-cycloserine against human neuroblastoma and medulloblastoma cells is associated with the suppression of ganglioside expression Anticancer Res. 19 , 5349-5354, (1999) 摘要
• Rath, G., et al., De novo ceramide synthesis is responsible for the anti-tumor properties of camptothecin and doxorubicin in follicular thyroid carcinoma. Int. J. Biochem. Cell Biol. 41 , 1165-72, (2009) 摘要
• Beil. 27 ,IV,5550

安全信息

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 2492 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NEPHBW Neuropharmacology.  (Pergamon Press Ltd., Headington Hill Hall,
   Oxford OX3 OBW, UK) V.9-    1970-  Volume(issue)/page/year: 25,411,1986

TYPE OF TEST            : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 2 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NEPHBW Neuropharmacology.  (Pergamon Press Ltd., Headington Hill Hall,
   Oxford OX3 OBW, UK) V.9-    1970-  Volume(issue)/page/year: 25,411,1986

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 1071 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NEPHBW Neuropharmacology.  (Pergamon Press Ltd., Headington Hill Hall,
   Oxford OX3 OBW, UK) V.9-    1970-  Volume(issue)/page/year: 25,411,1986

TYPE OF TEST            : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 500 mg/kg
TOXIC EFFECTS :
   Details of toxi

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 1889 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NEPHBW Neuropharmacology.  (Pergamon Press Ltd., Headington Hill Hall,
   Oxford OX3 OBW, UK) V.9-    1970-  Volume(issue)/page/year: 25,411,1986

其他信息

• MOL 文件:339-72-0.mol
• 制备方法:① 由放线菌经发酵、提炼及精制而成环丝氨酸。 ② 以丝氨酸甲酯的盐酸盐为原料，在五氯化磷的催化作用下，与三氯甲烷反应，脱羟基，再在氢氧化钠溶液中与羟胺反应，可制得环丝氨酸。
• Sigma Aldrich:339-72-
• Acros Organics:L-环丝氨酸 L-Cycloserine, 99%(339-72-0)
• 二线抗结核药:环丝氨酸属二线抗结核药，为广谱抗菌药物，对许多革兰阳性菌和阴性菌有较弱的抗菌作用。对结核杆菌具有抑制作用，抗结核杆菌作用远比异烟肼、链霉素弱，其抗菌机理是干扰细菌细胞壁的合成，抗结核杆菌的浓度为5～20mg/L，与其他抗结核药无交叉耐药性，细菌对之不易产生耐药性。由于对神经系统的毒性较大，仅用于其他药物治疗无效的患者。 口服吸收迅速，口服3～4小时达血药浓度峰值。口服一次0.25g达峰值平均为4mg/L，重复用药，可达到较高峰值。血浆半衰期为10小时。吸收后分布于全身组织、体液，可扩散进入胎儿循环和脑脊液、腹水、乳汁中。大部分以原形经肾排泄，肾功能不全者易蓄积中毒，小量从粪便中排出。 环丝氨酸的毒副作用主要为神经系统毒性反应。用药过程中如出现严重的精神症状，应立即停药。 从链丝菌培养液中提取的为D型，人工合成者为DL型光学异构体，临床所用环丝氨酸以后者为主，主要用于治疗结核病，特别适用于对其他抗结核药耐药的结核杆菌感染，常与其他抗结核药如异烟肼、链霉素和对氨基水杨酸等联用，也用于大肠杆菌所引起的尿路感染等。 信息由ChemicalBook的Andy编辑。
• 理化性质:白色或微红色晶体或粉末。有吸湿性。易潮解。味微酸。熔点155～156℃ (分解)，比旋光度+115°(c=1，水，22℃)、+137° (c=5，2mol/1NaOH)。易溶于水，溶于乙醇，微溶于氯仿、乙醚，不溶于一般有机溶剂。在碱性溶液中较为稳定，在酸性与中性溶液中则迅速分解。 环丝氨酸的抗菌谱广，除结核杆菌外，对大多数革兰阳性与阴性细菌、立克次体以及某些原虫等也都有抑制作用，对链霉素、紫霉素、对氨基水杨酸、异烟肼、吡嗪酰胺等耐药的结核杆菌也有作用。环丝氨酸与异烟肼对结核杆菌H37RV有轻度的协同作用，与链霉素既无协同亦不显示拮抗作用。本品为抑菌剂，增加剂量或延长与细菌作用时间，也不出现杀菌作用。本品抗菌作用的机理是抑制细菌细胞壁的合成。 环丝氨酸主要用于结核病，为二线药物，成人口服剂量为每日500mg，儿童为每日10mg/kg，均两次分服。重症病人可在短期内，增加剂量到每日1g。为了确保疗效又不致引起不良反应，在服药期间应定期测定血药浓度，以不超过30μg/ml为宜。同时服用巴比妥类药物，可减轻或防止惊厥发作。
• F:10
• L-Cycloserine is an irreversible inhibitor of 3-ketodihydrosphingosine synthetase, which is the first enzyme of the sphingolipid pathway, and causes the synthesis of sphingolipids to decrease. In vitro studies demonstrated that L-cyloserine inhibits 3-ketodihydrosphingosine synthetase 100 times more than D-Cycloserine .Research regarding L-Cycloserine and its effect on the immune response suggest that L-Cycloserine increases the level of IL-4 producing helper T cells and suppress the adhesion molecules CD29 and CD98. L-Cycloserine also inhibits SPTLC (serine palmitoyltransferase (SPT)), and HIV-1 investigations in the CD4+ lymphoid cell line (CEM) have shown that L-Cycloserine can inhibit HIV-1 replication.