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卡达唑胺
- names：
Cadazolid
- CAS号：
1025097-10-2
MDL Number： - MF(分子式)： C29H29F2N3O8 MW(分子量)： 585.55
- EINECS: Reaxys Number:
- Pubchem ID:44242317 Brand:BIOFOUNT
卡达唑胺(1025097-10-2,ACT-179811,Cadazolid)是一种新的恶唑烷酮类抗生素，对艰难梭菌具有有效的活性。
| 货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
|---|---|---|---|---|---|---|---|---|
| YZM000084-5mg | 5mg | 97.44% | ¥ 1072.50 | ¥ 1072.50 | 2-3天 | ¥ 0.00 |
| 中文别名 | 卡达唑胺(1025097-10-2);卡达唑利德;卡达唑烷; |
| 英文别名 | Cadazolid(1025097-10-2);Cadazolid;ACT 179811;ACT179811;ACT-179811;ACT-179811; ACT 179811; ACT179811; CADAZOLID.;Cadazolid (ACT-179811);CS-2475; |
| CAS号 | 1025097-10-2 |
| SMILES | O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4CCC(O)(COC5=CC=C(N6C(O[C@@H](CO)C6)=O)C=C5F)CC4)=C3)C1=O)O |
| Inchi | InChI=1S/C29H29F2N3O8/c30-21-10-19-23(33(16-1-2-16)13-20(26(19)36)27(37)38)11-24(21)32-7-5-29(40,6-8-32)15-41-25-4-3-17(9-22(25)31)34-12-18(14-35)42-28(34)39/h3-4,9-11,13,16,18,35,40H,1-2,5-8,12,14-15H2,(H,37,38)/t18-/m1/s1 |
| InchiKey | XWFCFMXQTBGXQW-GOSISDBHSA-N |
| 分子式 Formula | C29H29F2N3O8 |
| 分子量 Molecular Weight | 585.55 |
| 闪点 FP | 457.4±34.3 °C |
| 熔点 Melting point | No data available |
| 沸点 Boiling point | 832.6±65.0 °C at 760 mmHg |
| Polarizability极化度 | 55.7±0.5 10-24cm3 |
| 密度 Density | 1.5±0.1 g/cm3 |
| 蒸汽压 Vapor Pressure | 0.0±3.2 mmHg at 25°C |
| 溶解度Solubility | 生物体外In Vitro:DMSO溶解度≥ 150 mg/mL(256.17 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知. |
| 性状 | 固体粉末,Power |
| 储藏条件 Storage conditions | -20°C , 存放在阴凉干燥处,3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月 |
卡达唑胺(1025097-10-2,ACT-179811,Cadazolid)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
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| 产品说明 | 卡达唑胺(1025097-10-2,ACT-179811,Cadazolid)是一种有效的新的恶唑烷酮类抗生素，对Clostridium difficile具有有效的活性 |
| Introduction | 卡达唑胺(1025097-10-2,ACT-179811,Cadazolid)is a new oxazolidinone antibiotic with potent activity againstClostridium difficile. |
| Application1 | 卡达唑胺，也称为ACT-179811，是一种新的氟喹诺酮恶唑烷酮抗生素，对艰难梭菌具有有效活性。 |
| Application2 | |
| Application3 |
卡达唑胺(1025097-10-2,ACT-179811,Cadazolid)药理学：
卡达唑胺是恶唑烷酮类抗生素，对革兰氏阳性细菌（包括艰难梭菌）具有活性。尽管尚未完全阐明卡达唑利德发挥作用的确切作用方式，但在给药时，该药物抑制细菌蛋白质的合成并导致细菌细胞死亡。 卡达唑利德已用于研究艰难梭菌感染治疗的试验中。
卡达唑胺是恶唑烷酮类抗生素，对革兰氏阳性细菌（包括艰难梭菌）具有活性。尽管尚未完全阐明卡达唑利德发挥作用的确切作用方式，但在给药时，该药物抑制细菌蛋白质的合成并导致细菌细胞死亡。 卡达唑利德已用于研究艰难梭菌感染治疗的试验中。
| 警示图 | |
| 危险性 | warning |
| 危险性警示 | Not available |
| 安全声明 | H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害 |
| 安全防护 | P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理 |
| 备注 | 实验过程中防止吸入、食入，做好安全防护 |
| Baldoni D, et al. Cadazolid, a novel antibiotic with potent activity against Clostridium difficile: safety, tolerability and pharmacokinetics in healthy subjects following single and multiple oral dos |
| Chilton CH, et al. In vitro activity of cadazolid against clinically relevant Clostridium difficile isolates and in an in vitro gut model of C. difficile infection. J Antimicrob Chemother. 2014 Mar;69 |
| Cadazolid for the treatment of Clostridium difficile PMID 28286992; Expert opinion on investigational drugs 2017 Apr; 26(4):509-514 (Review Article) Name matches: surotomycin cadazolid |
| Novel Antimicrobials for the Treatment of Clostridium difficile Infection PMID 29713630; Frontiers in medicine 2018; 5(?):96 (Review Article) Name matches: surotomycin cadazolid |
| Management of adult Clostridium difficile digestive contaminations: a literature review PMID 30498879; European journal of clinical microbiology & infectious diseases : official publication of the Eur |
卡达唑胺(1025097-10-2,ACT-179811,Cadazolid)参考文献：
1.Novel Antimicrobials for the Treatment of
Petrosillo N;Granata G;Cataldo MA Front Med (Lausanne). 2018 Apr 16;5:96. doi: 10.3389/fmed.2018.00096. eCollection 2018.
The current picture of ;Clostridium difficile; infection (CDI) is alarming with a mortality rate ranging between 3% and 15% and a CDI recurrence rate ranging from 12% to 40%. Despite the great efforts made over the past 10 years to face the CDI burden, there are still gray areas in our knowledge on CDI management. The traditional anti-CDI antimicrobials are not always adequate in addressing the current needs in CDI management. The aim of our review is to give an update on novel antimicrobials for the treatment of CDI, considering the currently available evidences on their efficacy, safety, molecular mechanism of action, and their probability to be successfully introduced into the clinical practice in the near future. We identified, through a PubMed search, 16 novel antimicrobial molecules under study for CDI treatment: cadazolid, surotomycin, ridinilazole, LFF571, ramoplanin, CRS3123, fusidic acid, nitazoxanide, rifampin, rifaximin, tigecycline, auranofin, NVB302, thuricin CD, lacticin 3147, and acyldepsipeptide antimicrobials. In comparison with the traditional anti-CDI antimicrobial treatment, some of the novel antimicrobials reviewed in this study offer several advantages, i.e., the favorable pharmacokinetic and pharmacodynamic profile, the narrow-spectrum activity against CD that implicates a low impact on the gut microbiota composition, the inhibitory activity on CD sporulation and toxins production.
2.[New antibacterial agents on the market and in the pipeline].
Kern WV Internist (Berl). 2015 Nov;56(11):1255-63.
After some years of stagnation there have been several new successful developments in the field of antibacterial agents. Most of these new developments have been in conventional antibacterial classes. New drugs among the beta-lactam agents are methicillin-resistant Staphylococcus aureus (MRSA) active cephalosporins (ceftaroline and ceftobiprole) and new combinations of beta-lactam with beta-lactamase inhibitors (ceftolozane/tazobactam, ceftazidime/avibactam, imipenem/relebactam and meropenem/RPX7009). New developments can also be observed among oxazolidinones (tedizolid, radezolid, cadazolid and MRX-I), macrolides/ketolides (modithromycin and solithromycin), aminoglycosides (plazomicin), quinolones (nemonoxacin, delafloxacin and avarofloxacin), tetracyclines (omadacycline and eravacycline) as well as among glycopeptides and lipopeptides (oritavancin, telavancin, dalbavancin and surotomycin). New agents in a very early developmental phase are FabI inhibitors, endolysines, peptidomimetics, lipid A inhibitors, methionyl-tRNA synthetase inhibitors and teixobactin.
3.[Treatment of acute and recurrent Clostridium difficile infections : What is new?]
von Braun A;Lübbert C Internist (Berl). 2018 May;59(5):505-513. doi: 10.1007/s00108-018-0401-x.
The incidence of clostridium difficile infections (CDI) remains on a high level globally. In Germany, the number of severe or even lethal cases continues to increase. The main risk factor for the development of CDI is exposure to broad spectrum antibiotics, which disturb the physiological microbiome and therefore enable colonization with C. difficile. According to the updated US and European guidelines, orally administered vancomycin is the treatment of choice. Fidaxomicin is as effective as vancomycin but has the advantage of a lower rate of recurrence. Furthermore, recent clinical studies were able to demonstrate that significantly fewer recurrences occurred in patients who additionally received the monoclonal antibody bezlotoxumab. In recent years, several new antibiotics with narrow-spectrum acitivity and low intestinal resorption have been developed for the treatment of CDI, including surotomycin, cadazolid, and ridinilazol. Novel toxoid vaccines are expected to become an efficacious tool in the prevention of CDI; however, pivotal clinical trials have so far not been completed.
1.Novel Antimicrobials for the Treatment of
Petrosillo N;Granata G;Cataldo MA Front Med (Lausanne). 2018 Apr 16;5:96. doi: 10.3389/fmed.2018.00096. eCollection 2018.
The current picture of ;Clostridium difficile; infection (CDI) is alarming with a mortality rate ranging between 3% and 15% and a CDI recurrence rate ranging from 12% to 40%. Despite the great efforts made over the past 10 years to face the CDI burden, there are still gray areas in our knowledge on CDI management. The traditional anti-CDI antimicrobials are not always adequate in addressing the current needs in CDI management. The aim of our review is to give an update on novel antimicrobials for the treatment of CDI, considering the currently available evidences on their efficacy, safety, molecular mechanism of action, and their probability to be successfully introduced into the clinical practice in the near future. We identified, through a PubMed search, 16 novel antimicrobial molecules under study for CDI treatment: cadazolid, surotomycin, ridinilazole, LFF571, ramoplanin, CRS3123, fusidic acid, nitazoxanide, rifampin, rifaximin, tigecycline, auranofin, NVB302, thuricin CD, lacticin 3147, and acyldepsipeptide antimicrobials. In comparison with the traditional anti-CDI antimicrobial treatment, some of the novel antimicrobials reviewed in this study offer several advantages, i.e., the favorable pharmacokinetic and pharmacodynamic profile, the narrow-spectrum activity against CD that implicates a low impact on the gut microbiota composition, the inhibitory activity on CD sporulation and toxins production.
2.[New antibacterial agents on the market and in the pipeline].
Kern WV Internist (Berl). 2015 Nov;56(11):1255-63.
After some years of stagnation there have been several new successful developments in the field of antibacterial agents. Most of these new developments have been in conventional antibacterial classes. New drugs among the beta-lactam agents are methicillin-resistant Staphylococcus aureus (MRSA) active cephalosporins (ceftaroline and ceftobiprole) and new combinations of beta-lactam with beta-lactamase inhibitors (ceftolozane/tazobactam, ceftazidime/avibactam, imipenem/relebactam and meropenem/RPX7009). New developments can also be observed among oxazolidinones (tedizolid, radezolid, cadazolid and MRX-I), macrolides/ketolides (modithromycin and solithromycin), aminoglycosides (plazomicin), quinolones (nemonoxacin, delafloxacin and avarofloxacin), tetracyclines (omadacycline and eravacycline) as well as among glycopeptides and lipopeptides (oritavancin, telavancin, dalbavancin and surotomycin). New agents in a very early developmental phase are FabI inhibitors, endolysines, peptidomimetics, lipid A inhibitors, methionyl-tRNA synthetase inhibitors and teixobactin.
3.[Treatment of acute and recurrent Clostridium difficile infections : What is new?]
von Braun A;Lübbert C Internist (Berl). 2018 May;59(5):505-513. doi: 10.1007/s00108-018-0401-x.
The incidence of clostridium difficile infections (CDI) remains on a high level globally. In Germany, the number of severe or even lethal cases continues to increase. The main risk factor for the development of CDI is exposure to broad spectrum antibiotics, which disturb the physiological microbiome and therefore enable colonization with C. difficile. According to the updated US and European guidelines, orally administered vancomycin is the treatment of choice. Fidaxomicin is as effective as vancomycin but has the advantage of a lower rate of recurrence. Furthermore, recent clinical studies were able to demonstrate that significantly fewer recurrences occurred in patients who additionally received the monoclonal antibody bezlotoxumab. In recent years, several new antibiotics with narrow-spectrum acitivity and low intestinal resorption have been developed for the treatment of CDI, including surotomycin, cadazolid, and ridinilazol. Novel toxoid vaccines are expected to become an efficacious tool in the prevention of CDI; however, pivotal clinical trials have so far not been completed.
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