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400827-46-5
  • names:

    Ceftaroline fosamil

  • CAS号:

    400827-46-5

    MDL Number: MFCD19443689
  • MF(分子式): C24H25N8O10PS4 MW(分子量): 744.74
  • EINECS: Reaxys Number:
  • Pubchem ID:56841980 Brand:BIOFOUNT
头孢罗林酯
头孢罗林酯(400827-46-5,Ceftaroline fosamil,TAK-599)是一种能抗革兰氏阳性病原体包括耐甲氧西林金黄色葡萄球菌(MRSA)的头孢菌素。
货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
YZM000037-5mg 5mg 99.81% ¥ 2340.00 ¥ 2340.00 2-3天
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中文别名 头孢罗林酯(400827-46-5);头孢洛林酯;头孢罗林酯;PPI-0903;PPI0903;TAK-599;TAK599;特氟罗;
英文别名 Ceftaroline fosamill(400827-46-5);Zinforo;ceftaroline;fosamil;PPI-0903;PPI0903;TAK-599;TAK599;Teflaro;Teflaro; (6R,7R)-7-[[(2Z)-2-ethoxyimino-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl]amino]-3-[[4-(1-methylpyridin-1-ium-4-yl)-1,3-thiazol-2-yl]sulfanyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid,acetate; Ceftaroline fosamil; PPI 0903; Ceftaroline fosamil acetate anhydrous; UNII-EZ9W6O5S09; Zinforo; Ceftaroline fosamil acetate;
CAS号 400827-46-5
SMILES O=C1[C@@H](NC(/C(C2=NSC(NP(O)(O)=O)=N2)=N\OCC)=O)[C@@]3([H])SCC(SC4=NC(C5=CC=[N+](C)C=C5)=CS4)=C(C(O)=O)N13.CC([O-])=O
Inchi InChI=1S/C22H21N8O8PS4.C2H4O2/c1-3-38-26-13(16-25-21(43-28-16)27-39(35,36)37)17(31)24-14-18(32)30-15(20(33)34)12(9-40-19(14)30)42-22-23-11(8-41-22)10-4-6-29(2)7-5-10;1-2(3)4/h4-8,14,19H,3,9H2,1-2H3,(H4-,24,25,27,28,31,33,34,35,36,37);1H3,(H,3,4)/b26-13-;/t14-,19-;/m1./s1
InchiKey UGHHNQFYEVOFIV-VRDMTWHKSA-N
分子式 Formula C24H25N8O10PS4
分子量 Molecular Weight 744.74
闪点 FP
熔点 Melting point No data available
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility 生物体外In Vitro:DMSO溶解度30 mg/mL(40.28 mM;Need ultrasonic and warming)
性状 固体粉末,Power
储藏条件 Storage conditions -20°C 3 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

头孢罗林酯(400827-46-5,Ceftaroline fosamil,TAK-599)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.
Tags:TAK-599试剂,TAK-599杂质,TAK-599中间体,TAK-599合成,TAK-599密度,TAK-599溶解度,TAK-599旋光度,TAK-599购买,TAK-599闪点,TAK-599熔点,
产品说明 头孢罗林酯(400827-46-5,Ceftaroline fosamil,TAK-599)是一种能抗革兰氏阳性病原体包括耐甲氧西林金黄色葡萄球菌 (MRSA) 的头孢菌素
Introduction头孢罗林酯(400827-46-5,Ceftaroline fosamil,TAK-599)is a cephalosporin with activity againstGramositive pathogens, including methicillinesistantStaphylococcus aureus(MRSA).
Application1头孢洛林酯与一当量乙酸反应制得的乙酸盐。头孢洛林的前药,用于治疗患有急性细菌性皮肤和皮肤结构感染的成年人。
Application2Ceftaroline fosamil,也称为TAK 599,是一种头孢菌素抗生素,对耐甲氧西林的金黄色葡萄球菌(MRSA)和革兰氏阳性菌具有活性。Ceftaroline fosamil是头孢菌素抗生素T-91825的前药。
Application3
头孢罗林酯(400827-46-5,Ceftaroline fosamil,TAK-599)药理学:
1、头孢洛林Fosamil是具有抗菌活性的第五代头孢菌素衍生物头孢洛林的N-膦酰基前药。头孢洛林酯在体内被水解成头孢洛林的活性形式。头孢洛林与位于细菌细胞壁内膜上的青霉素结合蛋白(PBPs)结合并使其失活。PBP是参与细菌细胞壁组装以及在生长和分裂过程中重塑细胞壁末端阶段的酶。PBP的失活会干扰细菌细胞壁强度和刚度所必需的肽聚糖链的交联。这导致细菌细胞壁的弱化并引起细胞裂解。
2、Ceftaroline fosamil醋酸盐是ceftaroline fosamil的乙酸盐形式,ceftaroline fosamil是第五代头孢菌素衍生物ceftaroline的N-膦酰基型前药,具有抗菌活性。头孢洛林fosamil水解成头孢洛林的活性形式后,对青霉素结合蛋白2a(PBP2a)具有高亲和力,这与耐甲氧西林有关。结果,头孢洛林对耐甲氧西林,万古霉素,耐利奈唑胺和达托霉素的不敏感菌株具有独特的活性。
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
头孢罗林酯(400827-46-5,Ceftaroline fosamil,TAK-599)危害标识:
象形图
信号 Danger
GHS危险说明 Aggregated GHS information provided by 3 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
H317 (100%): May cause an allergic skin reaction [Warning Sensitization, Skin]
H334 (100%): May cause allergy or asthma symptoms or breathing difficulties if inhaled [Danger Sensitization, respiratory]
H400 (100%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard]
H410 (100%): Very toxic to aquatic life with long lasting effects [Warning Hazardous to the aquatic environment, long-term hazard]
Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范说明代码 P261, P272, P273, P280, P285, P302+P352, P304+P341, P321, P333+P313, P342+P311, P363, P391, and P501
(The corresponding statement to each P-code can be found at the GHS Classification page.)
 
Bhalodi AA, et al. Efficacy of ceftaroline fosamil in a staphylococcal murine pneumonia model. Antimicrob Agents Chemother. 2012 Dec;56(12):6160-5.
So W, et al. Comparison of in vivo and in vitro pharmacodynamics of a humanized regimen of 600 milligrams of Ceftaroline Fosamil every 12 hours against Staphylococcus aureus at initial inocula of 106
Ceftaroline fosamil: a novel broad-spectrum cephalosporin PMID 21076711; Drugs of today (Barcelona, Spain : 1998) 2010 Oct; 46(10):743-55 (Review Article) Name matches: cephalosporin ceftaroline fosam
Ceftaroline fosamil: a novel broad-spectrum cephalosporin with expanded anti-Gram-positive activity PMID 21115457; The Journal of antimicrobial chemotherapy 2010 Nov; 65 Suppl 4(?):iv9-16 (Review Arti
A Multicenter, Randomized, Observer-blinded, Active-controlled Study Evaluating the Safety and Effectiveness of Ceftaroline Compared With Ceftriaxone Plus Vancomycin in Pediatric Patients With Complic
头孢罗林酯(400827-46-5,Ceftaroline fosamil,TAK-599)参考文献:
1.In-use Stability of Ceftaroline Fosamil in Elastomeric Home Infusion Systems and MINI-BAG Plus Containers.
Bhattacharya S, Parekh S, Dedhiya M. Int J Pharm Compd. 2015 Sep-Oct;19(5):432-6.

The objective of this study was to determine in-use stability of ceftaroline fosamil infusion solution of concentrations up to 12 mg/mL in elastomeric home infusion system prefilled with 0.9% Sodium Chloride Injection USP or 5% Dextrose Injection USP and MINI-BAG Plus Container delivery devices prefilled with 0.9% sodium chloride injection. In-use ceftaroline fosamil infusion solution (12 mg/mL) was prepared for elastomeric home infusion systems (Homepump Eclipse, Baxter Intermate, and AccuRx Elastomeric Pump) pre-filled with either 0.9% sodium chloride injection or 5% dextrose; or Baxter MINI-BAG Plus Containers pre-filled with 0.9% Sodium Chloride Injection USP (4 mg/mL to 12 mg/mL ceftaroline fosamil in final solution). The systems were stored refrigerated for 24 hours followed by up to 6 hours of storage at room temperature. Samples were analyzed at various time points for assay and degradation product by a validated stability-indicating high-performance liquid chromatography method.

2.Single and repeated dose pharmacokinetics of ceftaroline in plasma and soft tissues of healthy volunteers for two different dosing regimens of ceftaroline fosamil.
Matzneller P1, Lackner E1, Lagler H2, Wulkersdorfer B1, Österreicher Z1, Zeitlinger M3. Antimicrob Agents Chemother. 2016 Apr 4. pii: AAC.00097-16. [Epub ahead of print]

OBJECTIVES: Ceftaroline fosamil (CPT-F) is currently approved for treatment of complicated skin and soft tissue infections and community-acquired pneumonia at 600 mg twice daily (q12h), but other dosing regimens are under evaluation. To date, very limited data on soft tissue pharmacokinetics (PK) of the active compound ceftaroline (CPT) are available.

3.Ceftaroline fosamil versus ceftriaxone for the treatment of community-acquired pneumonia: individual patient data meta-analysis of randomized controlled trials.
Taboada M1, Melnick D2, Iaconis JP3, Sun F4, Zhong NS5, File TM6, Llorens L7, Friedland HD7, Wilson D8. J Antimicrob Chemother. 2016 Apr;71(4):862-70. doi: 10.1093/jac/dkv415. Epub 2015 Dec 24.

BACKGROUND: We conducted a meta-analysis of clinical trials of adults hospitalized with pneumonia outcomes research team (PORT) risk class 3-4 community-acquired pneumonia (CAP) receiving ceftaroline fosamil versus ceftriaxone.

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