| 规格 | 价格 | 库存 | 数量 |
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| 靶点 |
DNA synthesis
Anaerobic bacterial DNA (MIC range: 0.125-8 μg/mL for Bacteroides fragilis group) [1][3] - Trichomonas vaginalis DNA (MIC = 0.25 μg/mL) [2] - Entamoeba histolytica DNA (MIC = 1 μg/mL) [2] - Giardia lamblia DNA (MIC = 0.5 μg/mL) [2] |
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| 体外研究 (In Vitro) |
甲硝唑在宿主或微生物细胞内代谢之前相对无活性。当甲硝唑收到来自铁氧还蛋白或黄伏氧还蛋白的电子时,甲硝唑被激活,该电子在厌氧或微需氧细菌或管腔寄生虫中被 POR 还原。甲硝唑通过形成蛋白质和 DNA 加合物来损害细胞。甲硝唑对溶组织阿米巴、贾第鞭毛虫和阴道毛滴虫等原生动物具有活性,该药物首次被批准作为有效治疗药物。甲硝唑对肠道厌氧菌群的活性已用于预防和治疗可能出现感染性并发症的克罗恩病患者。甲硝唑在厌氧菌相关感染中发挥着重要作用。甲硝唑对治疗厌氧性脑脓肿具有显着疗效。甲硝唑耐药性往往是由于驻留 rdxA 基因的从头突变引起的,而不是由于来自不相关但 Mtzr 菌株的突变 rdxA(或其他)基因的横向转移。甲硝唑部分抑制 rdxA(+)(甲硝唑(s))和 rdxA(甲硝唑(r))幽门螺杆菌菌株中利福平耐药性的生长刺激正向突变,并且 rdxA 在大肠杆菌中的表达导致等效的 Mtz 诱导突变。甲硝唑在纯人类杆菌的生长培养物中导致细胞凋亡样特征,包括程序性细胞死亡(PCD)的关键形态和生化特征,即。核浓缩和核内 DNA 缺口、细胞质体积减少、磷脂酰丝氨酸外化以及随着通透性增加而维持质膜完整性。
Metronidazole(甲硝唑)在厌氧条件下经细菌硝基还原酶(nim基因编码)激活,产生破坏细菌DNA链的硝基自由基,导致细胞死亡[1][3] - 针对脆弱拟杆菌临床分离株,Metronidazole 的MIC值为0.125-2 μg/mL,98%的菌株敏感(MIC ≤ 4 μg/mL)[1] - 对艰难梭菌菌株,Metronidazole 表现出抑制活性,MIC范围为0.5-4 μg/mL,可抑制孢子萌发和营养体生长[3] - 在阴道毛滴虫培养物中,Metronidazole(0.25 μg/mL)在孵育48小时内清除99%的滋养体[2] - 在浓度高达64 μg/mL时,对需氧菌(如大肠杆菌、金黄色葡萄球菌)无显著活性[1][3] - 耐Metronidazole的拟杆菌菌株(MIC > 32 μg/mL)表现出硝基还原酶活性降低和nimA基因过表达[1] |
| 体内研究 (In Vivo) |
甲硝唑(135 mg/kg/d;口服;28 d)可穿透血脑屏障,长期给予大鼠时会表现出神经毒性[3]。
甲硝唑(1 g/L;口服;28 d)可穿透血脑屏障。 po;4 周)会导致骨骼肌萎缩,并改变与代谢调节和肌肉外周昼夜节律机制相关的基因表达[4]。 在腹腔感染脆弱拟杆菌(1×10⁸ CFU/只)的小鼠中,口服Metronidazole(20 mg/kg,每日两次,连续5天)使腹腔液中细菌载量降低5 log10 CFU/mL,存活率从0%提高至90%[1] - 在艰难梭菌诱导的结肠炎大鼠模型中,Metronidazole(30 mg/kg,口服,每日三次,连续7天)缓解腹泻并减轻结肠黏膜炎症,粪便培养证实细菌清除[3] - 在阴道毛滴虫感染的小鼠中,Metronidazole(10 mg/kg,口服,每日一次,连续3天)在85%的动物中清除阴道滋养体[2] - 临床研究中,口服Metronidazole(250-500 mg,每日三次)治疗厌氧菌感染的治愈率为95%,治疗滴虫病的治愈率为90%[2] |
| 酶活实验 |
硝基还原酶激活实验:将重组细菌硝基还原酶(来自脆弱拟杆菌)与Metronidazole(0.1-10 μg/mL)及NADPH在厌氧缓冲液中37°C孵育30分钟。通过电子自旋共振(ESR)光谱检测硝基自由基代谢产物的生成[1][3]
- DNA损伤实验:将纯化的细菌DNA(脆弱拟杆菌)与激活的Metronidazole(由硝基还原酶+NADPH生成)在37°C孵育60分钟。通过琼脂糖凝胶电泳分析DNA链断裂,密度法定量损伤程度[1] - 厌氧菌MIC测定实验:在厌氧肉汤中制备Metronidazole的系列稀释液(0.0625-64 μg/mL),接种细菌悬液(5×10⁵ CFU/mL)。平板在37°C厌氧条件下孵育48小时,MIC定义为抑制可见生长的最低浓度[1][3] |
| 细胞实验 |
细胞系:芽囊菌 sp。细胞
浓度:0.1 μg/mL-0.01 mg/mL 孵育时间:12、24、48、60、72、84、96 小时 结果:细胞直径减小,作为凋亡的标志细胞,并导致细胞收缩。 阴道毛滴虫活力实验:将阴道毛滴虫滋养体以1×10⁵个/mL悬浮于培养基中,与Metronidazole(0.0625-4 μg/mL)在37°C孵育24-48小时。通过台盼蓝排斥法计数存活滋养体,计算MIC值[2] - 厌氧菌生长抑制实验:将脆弱拟杆菌或艰难梭菌与Metronidazole(0.1-32 μg/mL)在厌氧平板中培养48小时。计数菌落形成单位(CFU)以确定生长抑制率[1][3] - 耐药性实验:将耐Metronidazole和敏感的拟杆菌菌株在含0.5-16 μg/mL Metronidazole的培养基中培养72小时。通过分光光度法测定硝基还原酶活性,RT-PCR定量nimA基因表达[1] |
| 动物实验 |
Sprague-Dawley (SD) rats (200-220 g)
135 mg/kg Oral gavage; once daily; 28 days Bacteroides fragilis intraperitoneal infection model: Female Swiss mice (20-25 g) were infected intraperitoneally with 1×10⁸ CFU of B. fragilis. Metronidazole was dissolved in normal saline and administered orally at 10, 20, 40 mg/kg, twice daily for 5 days. Survival rate was recorded, and peritoneal fluid was collected for bacterial counting [1] - Clostridium difficile colitis model: Male Wistar rats (180-220 g) were pretreated with antibiotics to disrupt gut flora, then infected with C. difficile spores (1×10⁶ spores/rat) via oral gavage. Metronidazole (30 mg/kg) dissolved in 0.5% CMC-Na was administered orally three times daily for 7 days. Diarrhea score and colonic histopathology were evaluated [3] - Trichomonas vaginalis infection model: Female BALB/c mice (18-22 g) were infected intravaginally with T. vaginalis trophozoites (5×10⁴ cells/mouse). Metronidazole (10 mg/kg) dissolved in saline was administered orally once daily for 3 days. Vaginal washes were collected to detect viable trophozoites [2] |
| 药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
Following intravenous infusion of a 1.5g dose, peak concentrations are reached within 1 hour, with a peak concentration of 30-40 mg/L. After intravenous injection of 500mg three times daily, steady-state concentrations are reached after approximately 3 days, with a peak concentration of 26 mg/L. When taken orally as tablets, metronidazole is completely absorbed with a bioavailability greater than 90%. Data shows that the Cmax after a single oral dose of 500mg metronidazole is 8-13 mg/L, and the Tmax is 25 minutes to 4 hours. The AUC after a single oral dose of 500mg metronidazole is 122 ± 10.3 mg/L·h. Regarding absorption of topical formulations: After topical application of 1% metronidazole cream, transdermal absorption of metronidazole is negligible. In healthy volunteers, 100 mg of 14C-labeled 2% metronidazole cream was applied to intact skin. After 12 hours, metronidazole was not detected in plasma. The amount of metronidazole detected in urine and feces is approximately 0.1% to 1% of the administered dose. 60% to 80% of metronidazole and its metabolites are excreted in urine, and 6% to 15% in feces. Metronidazole is widely distributed throughout the body and in various body fluids, including bile, saliva, breast milk, cerebrospinal fluid, and the placenta. The steady-state volume of distribution of metronidazole in adults is 0.51 to 1.1 L/kg. Plasma concentrations of metronidazole in various tissues (e.g., the central nervous system) can reach 60% to 100%, but high concentrations have not been detected in placental tissue. Dosage adjustment may be necessary in patients with hepatic impairment due to reduced clearance. The renal clearance of metronidazole is estimated at 10 mL/min/1.73 m². Total serum clearance is approximately 2.1 to 6.4 L/h/kg. It is well absorbed orally; bioavailability is at least 80%. It is distributed in saliva, bile, semen, breast milk, bones, liver and liver abscesses, lungs, and vaginal secretions; it can also cross the placenta and blood-brain barrier. At least 80% of the oral dose of metronidazole is absorbed through the gastrointestinal tract. In healthy, fasting adults, after a single oral dose of 250 mg, 500 mg, or 2 g of immediate-release (conventional) metronidazole, peak plasma concentrations of the parent drug and its active metabolites are reached within 1–3 hours, with averages of 4.6–6.5 μg/mL, 11.5–13 μg/mL, and 30–45 μg/mL, respectively. In healthy, fasting adult women, after a single oral dose of 750 mg metronidazole (two 375 mg capsules or three 250 mg conventional tablets), average peak plasma concentrations of the parent drug and its active metabolites are reached within 1.4–1.6 hours, with an average of 20.4–21.4 μg/mL; at a single 750 mg dose, metronidazole capsules and conventional tablets are bioequivalent. Taking metronidazole tablets or capsules with food reduces its absorption and peak plasma concentration; however, the total amount of drug absorbed is not affected. In healthy adult women, after taking 750 mg of metronidazole extended-release tablets once daily for 7 consecutive days, the mean steady-state peak plasma concentration (MSP) was 12.5 μg/mL on an empty stomach, reaching an average of 6.8 hours after administration; when taking the same dose on a non-empty stomach, the mean MSP was 19.4 μg/mL, reaching an average of 4.6 hours after administration. Taking metronidazole extended-release tablets with food improves drug absorption and peak plasma concentration. According to the manufacturer, 750 mg metronidazole extended-release tablets and regular tablets are bioequivalent when taken on an empty stomach. For more complete data on the absorption, distribution, and excretion of metronidazole (12 types), please visit the HSDB record page. Metabolic/Metabolic Substances Metronidazole is metabolized in the liver via hydroxylation, oxidation, and glucuronidation. Metronidazole metabolism produces 5 metabolites. The hydroxy metabolite 1-(2-hydroxyethyl)-2-hydroxymethyl-5-nitroimidazole is considered the major active metabolite. Plasma contains unmetabolized metronidazole and a small amount of the 2-hydroxymethyl metabolite. Urine contains various metronidazole metabolites, primarily products of side-chain oxidation and glucuronide conjugation. Only 20% of metronidazole in urine is the unchanged drug. The two main oxidative metabolites of metronidazole are the hydroxy metabolite and the acetate metabolite. After oral or intravenous administration, approximately 30-60% of the drug is metabolized in the liver via hydroxylation, side-chain oxidation, and glucuronide conjugation. The major metabolite, 2-hydroxymetronidazole, possesses certain antibacterial and antiprobiotic activities. In addition, four nitro-containing metabolites were identified, all derived from the side-chain oxidation of ethyl and/or methyl groups. These metabolites include 1-acetic acid-2-methyl-5-nitroimidazole and 1-(2-hydroxyethyl)-2-carboxylic acid-5-nitroimidazole salts. The liver is the primary site of metronidazole metabolism, with a clearance rate exceeding 50%. The two main metabolites are produced by side-chain oxidation, resulting in hydroxyl derivatives and acids. The hydroxyl metabolite has a longer half-life (approximately 12 hours) and possesses nearly 50% of metronidazole's antitrichomonal activity. Furthermore, glucuronide formation has been observed. The gut microbiota produces small amounts of reducing metabolites, including ring-opening products. Some patients may experience reddish-brown urine due to the presence of an unknown pigment derived from the drug. Metabolism is primarily through hepatic hydroxylation, oxidation, and glucuronidation. Half-life: 6–8 hours. Following a single intravenous injection of 500 mg metronidazole in healthy subjects, the elimination half-life is 7.3 ± 1.0 hours. Another study indicated an elimination half-life of 6 to 10 hours. In adults with normal renal and hepatic function, the plasma half-life of metronidazole has been reported to be 6 to 8 hours. A study using radiolabeled metronidazole hydrochloride showed that the mean half-life of unmetabolized metronidazole was 7.7 hours, and the mean half-life of total radioactivity was 11.9 hours. The plasma half-life of metronidazole is not affected by changes in renal function; however, the half-life may be prolonged in patients with impaired liver function. A study in adults with alcoholic liver disease and impaired liver function showed that the mean half-life of metronidazole was 18.3 hours (range: 10.3 to 29.5 hours). Half-life: 25 to 75 hours in newborns; others: 6–8 hours, prolonged in cases of liver impairment. The elimination half-life in dogs is 4.5 hours, and in horses it is 1.5–3.3 hours. Oral bioavailability: After oral administration of 250-500 mg, the bioavailability in humans is 80-90% [2] -Plasma protein binding rate: 10-20% in human plasma (concentration range: 1-20 μg/mL) [2] -Metabolism: Metabolized by liver oxidation and glucuronidation, the main metabolite is 2-hydroxymetronidazole (active ingredient) [2] -Elimination half-life: 8-10 hours in humans; 4-6 hours in mice; 6-8 hours in rats [2] -Distribution: In humans, the volume of distribution (Vd) is 0.8-1.0 L/kg, widely distributed in tissues (liver, kidneys, brain, vaginal secretions) [2] -Excretion: 60-80% of the dose is excreted in urine as metabolites; 10-15% is excreted in feces; <5% Excreted in its original form [2] |
| 毒性/毒理 (Toxicokinetics/TK) |
Toxicity Summary
Metronidazole is a prodrug. Unionized metronidazole is selective for anaerobic bacteria because they can reduce it intracellularly to its active form. The reduced metronidazole then covalently binds to DNA, disrupting its helical structure, inhibiting bacterial nucleic acid synthesis, and ultimately leading to bacterial cell death. Toxicity Data LD50 = 500 mg/kg/day (oral administration in rats). Interactions Metronidazole should not be taken concurrently with alcohol, or at least within one day after alcohol consumption; interference with alcohol oxidation may lead to acetaldehyde accumulation, resulting in disulfiram-like effects such as abdominal cramps, nausea, vomiting, headache, or flushing; furthermore, it has been reported that the taste of alcoholic beverages may be altered when taken concurrently. When metronidazole is used concomitantly with coumarin or indanedione derivative anticoagulants, its effect may be enhanced because metronidazole inhibits the enzymatic metabolism of the anticoagulants; prothrombin time may need to be measured periodically during treatment to determine if the anticoagulant dose needs to be adjusted. When metronidazole is used concomitantly with cimetidine, hepatic metabolism of metronidazole may be reduced, which may lead to delayed clearance and elevated serum metronidazole concentrations; monitoring serum concentrations is recommended to guide dose adjustments, as the metronidazole dose may need to be adjusted during and after cimetidine treatment. It is recommended that patients with alcohol poisoning not take metronidazole and disulfiram concomitantly, or not take metronidazole concomitantly within 2 weeks after taking disulfiram. Such use may cause confusion and psychotic reactions due to combined toxicity. For more complete data on interactions of metronidazole (12 in total), please visit the HSDB records page. Non-human toxicity values Oral LD50 in albino rats > 5 g/kg Acute toxicity: Oral LD50 in mice = 1900 mg/kg; Oral LD50 in rats = 2500 mg/kg [2] -Gastrointestinal toxicity: Nausea (25%), vomiting (15%) and diarrhea (10%) occurred in humans; mild and reversible [2] -Neurotoxicity: Peripheral neuropathy (paresthesia, numbness) was reported in <5% of patients with long-term use (>2 weeks) or high doses (>2 g/day) [2] -Hepatotoxicity: Transient ALT/AST elevation occurred in <10% of patients; no significant hepatocellular damage was observed [2] -Disulfiram-like reaction: Flushing, tachycardia and hypotension (due to aldehyde dehydrogenase inhibition) occurred when used in combination with alcohol [2] -No significant nephrotoxicity was observed in patients with normal renal function [2] |
| 参考文献 | |
| 其他信息 |
Therapeutic Uses
MeSH Title: Anti-infectives, Antiprotozoal Drugs, Radiosensitizers Veterinary Drugs: Antiprotozoal Drugs (Trichomonas); Anti-amoebic Drugs; Antibacterial Drugs Veterinary Drugs: The success of metronidazole in treating giardiasis, vaginal and oral trichomoniasis, and hepatic and intestinal amebiasis in humans has prompted research into its potential use in treating certain protozoan diseases in livestock. These diseases primarily include bovine urogenital trichomoniasis and intestinal giardiasis, trichomoniasis, amebiasis, or Baramella infection in dogs, cats, or primates. ... Oral metronidazole (sustained-release formulation) is used to treat bacterial vaginosis caused by Gardnerella vaginalis, Animalia spp., Mycoplasma hominis, and anaerobic bacteria (Peptostreptococcus spp. and Bacteroides spp.). /Included on the product label in the US or Canada/ For more complete data on the therapeutic uses of metronidazole (25 in total), please visit the HSDB record page. Drug Warning Metronidazole can cross the placenta and rapidly enter fetal circulation. Adequate and well-controlled human studies have not been conducted. …However, metronidazole is not recommended for the treatment of trichomoniasis in early pregnancy. If metronidazole is used for trichomoniasis in mid-to-late pregnancy, it is recommended only for patients whose symptoms are not controlled by local palliative treatment. Furthermore, a 1-day course of treatment should not be used, as this can lead to excessively high maternal and fetal serum drug concentrations. There is currently no information regarding the relationship between age and the efficacy of metronidazole in elderly patients. However, elderly patients are more prone to age-related decline in liver function, which may require dose adjustment for patients receiving metronidazole. Peripheral neuropathy (manifested as numbness, tingling, or paresthesia in the limbs) and seizures have been reported rare after oral or intravenous administration of metronidazole. Peripheral neuropathy is usually reversible if metronidazole is discontinued, but it may persist in patients using the drug long-term or at doses higher than the recommended dose. Taking metronidazole may also cause symptoms such as dizziness, vertigo, incoordination, ataxia, confusion, irritability, depression, fatigue, insomnia, headache, syncope, tinnitus, and hearing loss. In non-pregnant women receiving oral metronidazole (extended-release tablets) for bacterial vaginosis, 18% experienced headaches, with 10% describing severe headaches. Oral metronidazole may also cause urethral burning or discomfort, difficulty urinating, cystitis, polyuria, urinary incontinence, pelvic pressure, vaginal or vulvar dryness, dyspareunia, and decreased libido. Due to water-soluble pigments produced by drug metabolism, urine may appear dark or reddish-brown after oral or intravenous administration of metronidazole. In a comparative study of treatments for bacterial vaginosis, 15% of non-pregnant women receiving oral metronidazole (extended-release tablets) reported vulvovaginal candidiasis (or yeast infection); while 12% of non-pregnant women receiving clindamycin phosphate (2% clindamycin) vaginal cream reported vulvovaginal candidiasis (or yeast infection). Although no clear causal relationship has been established with the drug, 5%, 3%, and 2% of non-pregnant women receiving oral metronidazole (extended-release tablets) for bacterial vaginosis reported genital itching, dysmenorrhea, and urinary tract infection, respectively. For more complete data on drug warnings for metronidazole (18 total), please visit the HSDB records page. Pharmacodynamics: Metronidazole is used to treat amebiasis, trichomoniasis, and giardiasis, and has antibacterial and antiprotozoal activity. Metronidazole is also effective against some anaerobic bacterial infections. Metronidazole exhibits antibacterial activity against most obligate anaerobes, but in vitro studies have shown that its antibacterial activity against facultative anaerobes or obligate aerobes is not significant. The reduction of the nitro group in metronidazole by anaerobic bacteria may be the cause of its antibacterial cytotoxic effect, leading to microbial DNA strand damage. Precautions regarding seizures, neuropathy, and carcinogenicity: The risk of peripheral neuropathy and seizures from metronidazole must be considered, especially at high doses. If seizures or limb numbness occur, the drug should be discontinued immediately. Metronidazole has been found to be carcinogenic in mice and rats, but its carcinogenicity in humans is not yet clear. Metronidazole should be used only when clinically necessary and solely for its approved indications. Metronidazole is a nitroimidazole antimicrobial drug with selective activity against anaerobic bacteria and protozoa[1][2][3] - Its mechanism of action requires anaerobic activation of bacterial/protozoal nitroreductase, which reduces nitro groups to form cytotoxic free radicals that damage DNA[1][3] - Indications include the treatment of anaerobic infections (intra-abdominal, pelvic, skin and soft tissue infections), Clostridium difficile-associated diarrhea, trichomoniasis, amebiasis and giardiasis[2] - Resistance is rare, but can be developed in Bacteroides through reduced nitroreductase activity or overexpression of the nim gene[1] - It is available in oral, intravenous and topical formulations; oral administration is preferred for mild to moderate infections[2] - Pregnancy category B (human data show no fetal risk), but caution is advised in early pregnancy[2] |
| 分子式 |
C6H9N3O3
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|---|---|---|
| 分子量 |
171.15
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| 精确质量 |
171.064
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| 元素分析 |
C, 42.10; H, 5.30; N, 24.55; O, 28.04
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| CAS号 |
443-48-1
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| 相关CAS号 |
1460293-84-8 (sodium); 13182-82-6 (acetate); 443-48-1 (free); 13182-89-3 (benzoate); 69198-10-3 (HCl); 443-48-1
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| PubChem CID |
4173
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| 外观&性状 |
White to light yellow crystalline powder
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| 密度 |
1.5±0.1 g/cm3
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|
| 沸点 |
405.4±25.0 °C at 760 mmHg
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| 熔点 |
159-161 °C(lit.)
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| 闪点 |
199.0±23.2 °C
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| 蒸汽压 |
0.0±1.0 mmHg at 25°C
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|
| 折射率 |
1.612
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|
| LogP |
-0.01
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| tPSA |
83.87
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|
| 氢键供体(HBD)数目 |
1
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| 氢键受体(HBA)数目 |
4
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| 可旋转键数目(RBC) |
2
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| 重原子数目 |
12
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| 分子复杂度/Complexity |
170
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|
| 定义原子立体中心数目 |
0
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| SMILES |
O([H])C([H])([H])C([H])([H])N1C(=C([H])N=C1C([H])([H])[H])[N+](=O)[O-]
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| InChi Key |
VAOCPAMSLUNLGC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H9N3O3/c1-5-7-4-6(9(11)12)8(5)2-3-10/h4,10H,2-3H2,1H3
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| 化学名 |
2-(2-methyl-5-nitroimidazol-1-yl)ethanol
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| 别名 |
|
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意: 本产品在运输和储存过程中需避光。 |
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| 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)
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| 溶解度 (体外实验) |
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|---|---|---|---|---|
| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.08 mg/mL (12.15 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 20.8 mg/mL澄清DMSO储备液加入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: ≥ 2.08 mg/mL (12.15 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 20.8 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: ≥ 2.08 mg/mL (12.15 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: 12.5 mg/mL (73.04 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 (<60°C). 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 | 5.8428 mL | 29.2141 mL | 58.4283 mL | |
| 5 mM | 1.1686 mL | 5.8428 mL | 11.6857 mL | |
| 10 mM | 0.5843 mL | 2.9214 mL | 5.8428 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) 。
Standard Versus Prolonged Antibiotic Prophylaxis After Pancreatoduodenectomy (SPARROW)
CTID: NCT05784311
Phase: Phase 4   Status: Recruiting
Date: 2024-10-21
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