| 规格 | 价格 | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| 体外研究 (In Vitro) |
pH值对新霉素B(又称新霉素B或夫雷霉素B)对RNase P RNA的抑制作用有影响,pH值升高会抵消其他系统的抑制作用[1]。人类和细胞核糖体翻译被新霉素B抑制。 5"-其氮基新霉素Fold B和新霉素B选择性抑制成熟miRNA的产生,增强转录因子,抑制HCC细胞系的右侧[2]。新霉素B与RNA的结构基序序列基序有主要同源性目标是16S rRNA解码位点,但它也与HIV-1锤头核酶、Rev反应元件和I族内含子结合,抑制它们的生物学功能[3]。这个过程导致误读遗传密码并抑制核糖体靶位点是 16 S rRNA 的 1400 至 1500 区域[4]。
|
|---|---|
| 药代性质 (ADME/PK) |
Metabolism / Metabolites
Neomycin undergoes minimal biotransformation after parenteral administration. Elimination Pathway: The small amount of absorbed drug is rapidly distributed in tissues and excreted via the kidneys, depending on renal function. Half-life: 2 to 3 hours |
| 毒性/毒理 (Toxicokinetics/TK) |
Toxicity Summary
Aminoglycoside antibiotics such as neomycin can bind "irreversibly" to specific 30S subunit proteins and 16S rRNA. Specifically, neomycin binds to four nucleotides of the 16S rRNA and one amino acid of the S12 protein. This interferes with the decoding site near nucleotide 1400 in the 30S subunit 16S rRNA. This region interacts with the wobble base in the tRNA anticodon. This leads to interference with the initiation complex, mRNA misreading, resulting in the insertion of incorrect amino acids into the polypeptide chain, leading to the production of nonfunctional or toxic peptides, and the breakdown of polyribosomes into nonfunctional monomeric ribosomes. Pregnancy and Lactation Effects ◉ Overview of Lactation Use While there is currently no information regarding the secretion of neomycin into breast milk, the amount of other aminoglycoside antibiotics secreted into breast milk is minimal. Newborns appear to absorb small amounts of aminoglycoside antibiotics, but their serum concentrations are far lower than those achieved when treating neonatal infections, making systemic effects of neomycin unlikely. Older infants are expected to absorb less neomycin. Closely monitor the infant's gut microbiota for potential effects such as diarrhea, candidiasis (e.g., thrush, diaper rash), or rare hematochezia, which may indicate antibiotic-associated colitis. Oral, topical, ophthalmic, or otopathic neomycin concentrations in breast milk should be extremely low, posing negligible risk to the infant; however, nipple application may increase the risk of diarrhea in the infant. Only water-soluble creams or gels should be applied to the breast, as ointments may expose the infant to high concentrations of mineral oil through licking. ◉ Effects on breastfed infants: No published information found as of the revision date. ◉ Effects on lactation and breast milk: No published information found as of the revision date. Toxicity Data LD50: 200 mg/kg (rat) (A308) |
| 参考文献 |
|
| 其他信息 |
Framycetin is a tetracyclic antibacterial agent derived from neomycin, and is a glycoside ester of neomycin amine and neomycin B. It possesses multiple functions, including antibacterial activity, allergen status, and being a metabolite of E. coli. It is the conjugate base of Framycetin (6+). Neomycin is produced by Streptomyces fradiae. Hydrolysis yields neomycin amine and neomycin B. (From Merck Index, 11th edition) Neomycin has also been reported in soybean (Glycine max), Streptomyces albus, and other microorganisms with relevant data. Framycetin is an aminoglycoside antibiotic isolated from Streptomyces lavendulae (decaris), with neomycin B as its main component, exhibiting broad-spectrum antibacterial activity. Framycetin is primarily used as a topical preparation, with low absorption. Parenteral administration can cause nephrotoxicity and ototoxicity. Neomycin is a component of Streptomyces fradiae. Hydrolysis yields neomycin amine and neomycin B. (From Merck Index, 11th edition). Neomycin is a bactericidal aminoglycoside antibiotic that binds to the 30S ribosomes of susceptible bacteria. This binding interferes with both the mRNA binding site and the receptor tRNA site, resulting in the production of nonfunctional or toxic peptides. See also: Neomycin (note moved to) Neomycin sulfate (note moved to).
Indications For the treatment of bacterial blepharitis, bacterial conjunctivitis, corneal injury, corneal ulceration, and meibomianitis. For the prevention of ocular infection after foreign body removal. Mechanism of Action Flamexetine binds to specific 30S subunit proteins and 16S rRNA, binding four nucleotides of the 16S rRNA and one amino acid of the S12 protein. This interferes with the decoding site near nucleotide 1400 in the 30S subunit 16S rRNA. This region interacts with the wobble base in the tRNA anticodon. This leads to interference with the initiation complex, misreading of the mRNA, inserting incorrect amino acids into the polypeptide chain, producing nonfunctional or toxic peptides, and causing polyribosomes to break down into nonfunctional monomeric ribosomes. Pharmacodynamics Flamexetine is used to treat bacterial eye infections, such as conjunctivitis. Flamexetine is an antibiotic. It is ineffective against fungi, viruses, and most anaerobes. Flamexetine's mechanism of action is to bind to the bacterial 30S ribosomal subunit, causing tRNA misreading and preventing the bacteria from synthesizing proteins essential for their growth. Flamexetine is primarily used to treat aerobic bacterial infections. |
| 分子式 |
C23H46N6O13
|
|---|---|
| 分子量 |
614.64374
|
| 精确质量 |
614.312
|
| CAS号 |
119-04-0
|
| 相关CAS号 |
Framycetin sulfate;4146-30-9;Neomycin sulfate;1405-10-3
|
| PubChem CID |
8378
|
| 外观&性状 |
Colorless to light yellow liquid
|
| 密度 |
1.61 g/cm3
|
| 沸点 |
927.1ºC at 760 mmHg
|
| 熔点 |
6 °C (sulfate form)
|
| 闪点 |
514.5ºC
|
| 折射率 |
1.6000 (estimate)
|
| LogP |
-9
|
| tPSA |
353.11
|
| 氢键供体(HBD)数目 |
13
|
| 氢键受体(HBA)数目 |
19
|
| 可旋转键数目(RBC) |
9
|
| 重原子数目 |
42
|
| 分子复杂度/Complexity |
872
|
| 定义原子立体中心数目 |
19
|
| SMILES |
C1[C@H]([C@@H]([C@H]([C@@H]([C@H]1N)O[C@@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CN)O)O)N)O[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O[C@@H]4[C@@H]([C@H]([C@@H]([C@@H](O4)CN)O)O)N)O)O)N
|
| InChi Key |
PGBHMTALBVVCIT-KNSIFCLBSA-N InChi Code
|
| InChi Code |
InChI=1S/C23H46N6O13/c24-2-7-13(32)15(34)10(28)21(37-7)40-18-6(27)1-5(26)12(31)20(18)42-23-17(36)19(9(4-30)39-23)41-22-11(29)16(35)14(33)8(3-25)38-22/h5-23,30-36H,1-4,24-29H2/t5-,6+,7-,8+,9-,10-,11-,12+,13-,14-,15-,16-,17-,18-,19-,20-,21-,22-,23+/m1/s1
|
| 化学名 |
(2S,3S,4R,5R,6R)-5-amino-2-(aminomethyl)-6-(((2R,3S,4R,5S)-5-(((1R,2R,3S,5R,6S)-3,5-diamino-2-(((2R,3R,4R,5R,6R)-3-amino-6-(aminomethyl)-4,5-dihydroxytetrahydro-2H-pyran-2-yl)oxy)-6-hydroxycyclohexyl)oxy)-4-hydroxy-2-(hydroxymethyl)tetrahydrofuran-3-yl)oxy)tetrahydro-2H-pyran-3,4-diol
|
| 别名 |
Neomycin B Fradiomycin B Actilin Soframycin
|
| HS Tariff Code |
2934.99.9001
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外实验) |
H2O : ~100 mg/mL (~162.70 mM)
DMSO : ~50 mg/mL (~81.35 mM) |
|---|---|
| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (4.07 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (4.07 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (4.07 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 配方 4 中的溶解度: 120 mg/mL (195.24 mM) in PBS (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液; 超声助溶. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6270 mL | 8.1348 mL | 16.2697 mL | |
| 5 mM | 0.3254 mL | 1.6270 mL | 3.2539 mL | |
| 10 mM | 0.1627 mL | 0.8135 mL | 1.6270 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
Decolonization of Carbapenem-resistant Enterobacterales (CRE) in Patients With Faecal Carriage of CRE With Neomycin
CTID: NCT05593601
Phase: Phase 4   Status: Unknown status
Date: 202
Intestinal colonization by multiresistant enterobacteria in patients with kidney and liver transplantation: multicentre cohort study and randomized, controlled, open clinical trial.
CTID: null
Phase: Phase 4   Status: Ongoing
Date: 2014-08-13