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頭孢羅林酯

NMR下載 COA and HPLC MSDS下載
names：
Ceftaroline fosamil
CAS號：
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

頭孢羅林酯(400827-46-5,Ceftaroline fosamil,TAK-599)是一種能抗革蘭氏陽性病原體包括耐甲氧西林金黃色葡萄球菌（MRSA）的頭孢菌素。

貨品編碼	規(guī)格	純度	價格 (￥)	現(xiàn)價(￥)	特價(￥)	庫存描述	數(shù)量	總計 (￥)
YZM000037-5mg	5mg	99.81%	￥ 2340.00	￥ 2340.00		2-3天	- +	￥ 0.00

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中文別名	頭孢羅林酯(400827-46-5);頭孢洛林酯;頭孢羅林酯;PPI-0903;PPI0903;TAK-599;TAK599;特氟羅;
英文別名	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號	400827-46-5
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
溶解度Solubility	生物體外In Vitro:DMSO溶解度30 mg/mL(40.28 mM;Need ultrasonic and warming)
性狀	固體粉末,Power
儲藏條件 Storage conditions	-20°C 3 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

頭孢羅林酯(400827-46-5,Ceftaroline fosamil,TAK-599)實驗注意事項：
1.實驗前需戴好防護(hù)眼鏡，穿戴防護(hù)服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)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試劑,TAK-599雜質(zhì),TAK-599中間體,TAK-599合成,TAK-599密度,TAK-599溶解度,TAK-599旋光度,TAK-599購買,TAK-599閃點,TAK-599熔點,

產(chǎn)品說明	頭孢羅林酯(400827-46-5,Ceftaroline fosamil,TAK-599)是一種能抗革蘭氏陽性病原體包括耐甲氧西林金黃色葡萄球菌 (MRSA) 的頭孢菌素
Introduction	頭孢羅林酯(400827-46-5,Ceftaroline fosamil,TAK-599)is a cephalosporin with activity againstGramositive pathogens, including methicillinesistantStaphylococcus aureus(MRSA).
Application1	頭孢洛林酯與一當(dāng)量乙酸反應(yīng)制得的乙酸鹽。頭孢洛林的前藥，用于治療患有急性細(xì)菌性皮膚和皮膚結(jié)構(gòu)感染的成年人。
Application2	Ceftaroline fosamil，也稱為TAK 599，是一種頭孢菌素抗生素，對耐甲氧西林的金黃色葡萄球菌（MRSA）和革蘭氏陽性菌具有活性。Ceftaroline fosamil是頭孢菌素抗生素T-91825的前藥。
Application3

頭孢羅林酯(400827-46-5,Ceftaroline fosamil,TAK-599)藥理學(xué)：

1、頭孢洛林Fosamil是具有抗菌活性的第五代頭孢菌素衍生物頭孢洛林的N-膦酰基前藥。頭孢洛林酯在體內(nèi)被水解成頭孢洛林的活性形式。頭孢洛林與位于細(xì)菌細(xì)胞壁內(nèi)膜上的青霉素結(jié)合蛋白（PBPs）結(jié)合并使其失活。PBP是參與細(xì)菌細(xì)胞壁組裝以及在生長和分裂過程中重塑細(xì)胞壁末端階段的酶。PBP的失活會干擾細(xì)菌細(xì)胞壁強(qiáng)度和剛度所必需的肽聚糖鏈的交聯(lián)。這導(dǎo)致細(xì)菌細(xì)胞壁的弱化并引起細(xì)胞裂解。

2、Ceftaroline fosamil醋酸鹽是ceftaroline fosamil的乙酸鹽形式，ceftaroline fosamil是第五代頭孢菌素衍生物ceftaroline的N-膦?；颓八?，具有抗菌活性。頭孢洛林fosamil水解成頭孢洛林的活性形式后，對青霉素結(jié)合蛋白2a（PBP2a）具有高親和力，這與耐甲氧西林有關(guān)。結(jié)果，頭孢洛林對耐甲氧西林，萬古霉素，耐利奈唑胺和達(dá)托霉素的不敏感菌株具有獨特的活性。

警示圖
危險性	warning
危險性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害
安全防護(hù)	P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護(hù)理
備注	實驗過程中防止吸入、食入，做好安全防護(hù)

頭孢羅林酯(400827-46-5,Ceftaroline fosamil,TAK-599)危害標(biāo)識：

象形圖




信號	Danger
GHS危險說明	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.
防范說明代碼	P261, P272, P273, P280, P285, P302+P352, P304+P341, P321, P333+P313, P342+P311, P363, P391, and P501
防范說明代碼	(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

頭孢羅林酯(400827-46-5,Ceftaroline fosamil,TAK-599)參考文獻(xiàn)：

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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