購(gòu)物車(chē) 
-
拉諾培登
- names：
Lanopepden
- CAS號(hào)：
1152107-25-9
MDL Number： MFCD20526985 - MF(分子式)： C22H34FN7O4 MW(分子量)： 479.55
- EINECS:629-881-5 Reaxys Number:
- Pubchem ID:52918384 Brand:BIOFOUNT
拉諾培登(1152107-25-9,Lanopepden,GSK 1322322)是一種肽去甲酰胺酶抑制劑，GSK 1322322可抑制金黃色葡萄球菌。GSK 1322322抑制ATCC 29213和ATCC 25923甲苯，MIC都為1 mg / L。
| 貨品編碼 | 規(guī)格 | 純度 | 價(jià)格 (￥) | 現(xiàn)價(jià)(￥) | 特價(jià)(￥) | 庫(kù)存描述 | 數(shù)量 | 總計(jì) (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000166-1mg | 1mg | >97% | ￥ 3412.50 | ￥ 3412.50 | 2-3天 | ￥ 0.00 |
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| 中文別名 | 拉諾培登(1152107-25-9);拉諾培登 ;N-[（2R）-2-（環(huán)戊基甲基）-3-（2- {5-氟-6-[（9aS）-六氫吡嗪并[2,1-c] [1,4]惡嗪-8（1H）-酰基]-2-甲基嘧啶-4-基}肼-1-基）-3-氧丙基]-N-羥基甲酰胺，GSK-1322322，GSK-322； |
| 英文別名 | Lanopepden(1152107-25-9);GSK1322322;N-[(2R)-2-(cyclopentylmethyl)-3-(2-{5-fluoro- 6-[(9aS)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]- 2-methylpyrimidin-4-yl}hydrazin-1-yl)-3-oxopropyl]- N-hydroxyformamide,GSK-1322322,GSK-322; |
| CAS號(hào) | 1152107-25-9 |
| Inchi | InChI=1S/C22H34FN7O4/c1-15-24-20(19(23)21(25-15)29-7-6-28-8-9-34-13-18(28)12-29)26-27-22(32)17(11-30(33)14-31)10-16-4-2-3-5-16/h14,16-18,33H,2-13H2,1H3,(H,27,32)(H,24,25,26)/t17-,18+/m1/s1 |
| InchiKey | SWHNZGMQMGFQGW-MSOLQXFVSA-N |
| 分子式 Formula | C22H34FN7O4 |
| 分子量 Molecular Weight | 479.55 |
| 溶解度Solubility | |
| 性狀 | 固體粉末,Power |
| 儲(chǔ)藏條件 Storage conditions | -20°C Freezer,3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月 |
拉諾培登(1152107-25-9,Lanopepden,GSK 1322322)實(shí)驗(yàn)注意事項(xiàng)：
1.實(shí)驗(yàn)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(shí)驗(yàn)過(guò)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(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類(lèi)存儲(chǔ)，并交于專(zhuān)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:拉諾培登試劑,拉諾培登雜質(zhì),拉諾培登合成,拉諾培登密度,拉諾培登溶解度,拉諾培登旋光度,拉諾培登閃點(diǎn),拉諾培登熔點(diǎn),拉諾培登購(gòu)買(mǎi),拉諾培登MSDS,
| 產(chǎn)品說(shuō)明 | 拉諾培登(1152107-25-9,Lanopepden,GSK 1322322)是一種肽去甲酰基酶抑制劑,對(duì)金黃色葡萄球菌菌株具有活性 |
| Introduction | 拉諾培登(1152107-25-9,Lanopepden,GSK 1322322)is a peptide deformylase inhibitor active againstStaphylococcus aureusstrains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively. |
| Application1 | 拉諾培登(1152107-25-9,Lanopepden,GSK 1322322)對(duì)ATCC 29213和ATCC 25923菌株的MIC分別為1和1 mg / L，已用于研究治療肺炎，感染，細(xì)菌，皮膚病，感染和皮膚感染，細(xì)菌的試驗(yàn)中。 |
| Application2 | |
| Application3 |
拉諾培登(1152107-25-9,Lanopepden,GSK 1322322)藥理學(xué)：
1、該活性分子是選擇性肽去甲?；敢种苿?。在體外具有良好的抗菌活性。Lanopepden的抗菌譜包括肺炎鏈球菌，流感嗜血桿菌，化膿性鏈球菌和金黃色葡萄球菌，這表明在29個(gè)月的24小時(shí)內(nèi)，在4×MIC下CFU / ml的數(shù)量降低了≥3-log（10）。測(cè)試了33個(gè)菌株。它也可以用于治療由耐藥菌引起的傳染病。2015年1月1日，葛蘭素史克（GlaxoSmithKline）撤回了美國(guó)細(xì)菌感染的I期試驗(yàn)。2015年1月26日，葛蘭素史克（GlaxoSmithKline）撤回了美國(guó)健康志愿者的第一階段藥代動(dòng)力學(xué)/藥效學(xué)試驗(yàn)。
2、Lanopepden（GSK 1322322）是一種肽去甲酰基酶抑制劑，對(duì)金黃色葡萄球菌菌株具有活性，對(duì)ATCC 29213和ATCC 25923菌株的MIC分別為1和1 mg / L。
1、該活性分子是選擇性肽去甲?；敢种苿?。在體外具有良好的抗菌活性。Lanopepden的抗菌譜包括肺炎鏈球菌，流感嗜血桿菌，化膿性鏈球菌和金黃色葡萄球菌，這表明在29個(gè)月的24小時(shí)內(nèi)，在4×MIC下CFU / ml的數(shù)量降低了≥3-log（10）。測(cè)試了33個(gè)菌株。它也可以用于治療由耐藥菌引起的傳染病。2015年1月1日，葛蘭素史克（GlaxoSmithKline）撤回了美國(guó)細(xì)菌感染的I期試驗(yàn)。2015年1月26日，葛蘭素史克（GlaxoSmithKline）撤回了美國(guó)健康志愿者的第一階段藥代動(dòng)力學(xué)/藥效學(xué)試驗(yàn)。
2、Lanopepden（GSK 1322322）是一種肽去甲酰基酶抑制劑，對(duì)金黃色葡萄球菌菌株具有活性，對(duì)ATCC 29213和ATCC 25923菌株的MIC分別為1和1 mg / L。
| 警示圖 | |
| 危險(xiǎn)性 | warning |
| 危險(xiǎn)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(duì)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(shí)驗(yàn)過(guò)程中防止吸入、食入，做好安全防護(hù) |
拉諾培登(1152107-25-9,Lanopepden,GSK 1322322)危害標(biāo)識(shí)：
| 象形圖 |  |
| 信號(hào) | Warning |
| GHS危險(xiǎn)說(shuō)明 | The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory. |
| H373 (100%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure] | |
| 防范說(shuō)明代碼 | P260, P314, and P501 |
| (The corresponding statement to each P-code can be found at the GHS Classification page.) |
| Peyrusson F, et al. Cellular pharmacokinetics and intracellular activity of the novel peptide deformylase inhibitor GSK1322322 against Staphylococcus aureus laboratory and clinical strains with variou |
| Pharmacokinetics/Pharmacodynamics of Peptide Deformylase Inhibitor GSK1322322 against Streptococcus pneumoniae, Haemophilus influenzae, and Staphylococcus aureus in Rodent Models of Infection PMID 264 |
| Determination of disk diffusion and MIC quality control ranges for GSK1322322, a novel peptide deformylase inhibitor PMID 21918031; Journal of clinical microbiology 2011 Nov; 49(11):3928-30 Name match |
| Single-dose safety, tolerability, and pharmacokinetics of the antibiotic GSK1322322, a novel peptide deformylase inhibitor PMID 23403431; Antimicrobial agents and chemotherapy 2013 May; 57(5):2005-9 N |
| Comparative analysis of the antibacterial activity of a novel peptide deformylase inhibitor, GSK1322322 PMID 23478958; Antimicrobial agents and chemotherapy 2013 May; 57(5):2333-42 Name matches: beta- |
拉諾培登(1152107-25-9,Lanopepden,GSK 1322322)參考文獻(xiàn)：
1.Investigation of metabolism and disposition of GSK1322322, a peptidase deformylase inhibitor, in healthy humans using the entero-test for biliary sampling.
Mamaril-Fishman D;Zhu J;Lin M;Felgate C;Jones L;Stump P;Pierre E;Bowen C;Naderer O;Dumont E;Patel P;Gorycki PD;Wen B;Chen L;Deng Y Drug Metab Dispos. 2014 Aug;42(8):1314-25. doi: 10.1124/dmd.114.058420. Epub 2014 May 28.
GSK1322322 (N-((R)-2-(cyclopentylmethyl)-3-(2-(5-fluoro-6-((S)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl)-2-methylpyrimidin-4-yl)hydrazinyl)-3-oxopropyl)-N-hydroxy-formamide) is an antibiotic in development by GlaxoSmithKline. In this study, we investigated the metabolism and disposition of [(14)C]GSK1322322 in healthy humans and demonstrated the utility of the Entero-Test in a human radiolabel study. We successfully collected bile from five men using this easy-to-use device after single i.v. (1000 mg) or oral administration (1200 mg in a solution) of [(14)C]GSK1322322. GSK1322322 had low plasma clearance (23.6 liters/hour) with a terminal elimination half-life of ∼4 hours after i.v. administration. After oral administration, GSK1322322 was readily and almost completely absorbed (time of maximal concentration of 0.5 hour; bioavailability 97%). GSK1322322 predominated in the systemic circulation (>64% of total plasma radioactivity). An O-glucuronide of GSK1322322 (M9) circulated at levels between 10% and 15% of plasma radioactivity and was pharmacologically inactive. Humans eliminated the radioactive dose in urine and feces at equal proportions after both i.v. and oral doses (∼45%-48% each).
2.Potent sub-MIC effect of GSK1322322 and other peptide deformylase inhibitors on in vitro growth of Staphylococcus aureus.
Butler D;Chen D;O'Dwyer K;Lewandowski T;Aubart K;Zalacain M Antimicrob Agents Chemother. 2014;58(1):290-6. doi: 10.1128/AAC.01292-13. Epub 2013 Oct 28.
Peptide deformylase (PDF), a clinically unexploited antibacterial target, plays an essential role in protein maturation. PDF inhibitors, therefore, represent a new antibiotic class with a unique mode of action that provides an alternative therapy for the treatment of infections caused by drug-resistant pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). GSK1322322 is a novel PDF inhibitor that is in phase II clinical development for the treatment of lower respiratory tract and skin infections. We have discovered that PDF inhibitors can prevent S. aureus in vitro growth for up to 6 h at concentrations 8- to 32-fold below their MICs. This phenomenon seems specific to PDF inhibitors, as none of the antimicrobial agents with alternative mechanisms of action tested show such a potent and widespread effect. It also appears limited to S. aureus, as PDF inhibitors do not show such an inhibition of growth at sub-MIC levels in Streptococcus pneumoniae or Haemophilus influenzae. Analysis of the effect of GSK1322322 on the early growth of 100 randomly selected S. aureus strains showed that concentrations equal to or below 1/8× MIC inhibited growth of 91% of the strains tested for 6 h, while the corresponding amount of moxifloxacin or linezolid only affected the growth of 1% and 6% of strains, respectively.
3.Comparative analysis of the antibacterial activity of a novel peptide deformylase inhibitor, GSK1322322.
O'Dwyer K;Hackel M;Hightower S;Hoban D;Bouchillon S;Qin D;Aubart K;Zalacain M;Butler D Antimicrob Agents Chemother. 2013 May;57(5):2333-42. doi: 10.1128/AAC.02566-12. Epub 2013 Mar 11.
GSK1322322 is a novel peptide deformylase (PDF) inhibitor being developed for the intravenous and oral treatment of acute bacterial skin and skin structure infections and hospitalized patients with community-acquired pneumonia. The activity of GSK1322322 was tested against a global collection of clinical isolates of Haemophilus influenzae (n = 2,370), Moraxella catarrhalis (n = 115), Streptococcus pneumoniae (n = 947), Streptococcus pyogenes (n = 617), and Staphylococcus aureus (n = 940), including strains resistant to one or more marketed antibiotics. GSK1322322 had an MIC(90) of 1 μg/ml against M. catarrhalis and 4 μg/ml against H. influenzae, with 88.8% of β-lactamase-positive strains showing growth inhibition at that concentration. All S. pneumoniae strains were inhibited by ≤ 4 μg/ml of GSK1322322, with an MIC(90) of 2 μg/ml. Pre-existing resistance mechanisms did not affect its potency, as evidenced by the MIC(90) of 1 μg/ml for penicillin, levofloxacin, and macrolide-resistant S. pneumoniae. GSK1322322 was very potent against S. pyogenes strains, with an MIC(90) of 0.5 μg/ml, irrespective of their macrolide resistance phenotype. This PDF inhibitor was also active against S. aureus strains regardless of their susceptibility to methicillin, macrolides, or levofloxacin, with an MIC(90) of 4 μg/ml in all cases.
1.Investigation of metabolism and disposition of GSK1322322, a peptidase deformylase inhibitor, in healthy humans using the entero-test for biliary sampling.
Mamaril-Fishman D;Zhu J;Lin M;Felgate C;Jones L;Stump P;Pierre E;Bowen C;Naderer O;Dumont E;Patel P;Gorycki PD;Wen B;Chen L;Deng Y Drug Metab Dispos. 2014 Aug;42(8):1314-25. doi: 10.1124/dmd.114.058420. Epub 2014 May 28.
GSK1322322 (N-((R)-2-(cyclopentylmethyl)-3-(2-(5-fluoro-6-((S)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl)-2-methylpyrimidin-4-yl)hydrazinyl)-3-oxopropyl)-N-hydroxy-formamide) is an antibiotic in development by GlaxoSmithKline. In this study, we investigated the metabolism and disposition of [(14)C]GSK1322322 in healthy humans and demonstrated the utility of the Entero-Test in a human radiolabel study. We successfully collected bile from five men using this easy-to-use device after single i.v. (1000 mg) or oral administration (1200 mg in a solution) of [(14)C]GSK1322322. GSK1322322 had low plasma clearance (23.6 liters/hour) with a terminal elimination half-life of ∼4 hours after i.v. administration. After oral administration, GSK1322322 was readily and almost completely absorbed (time of maximal concentration of 0.5 hour; bioavailability 97%). GSK1322322 predominated in the systemic circulation (>64% of total plasma radioactivity). An O-glucuronide of GSK1322322 (M9) circulated at levels between 10% and 15% of plasma radioactivity and was pharmacologically inactive. Humans eliminated the radioactive dose in urine and feces at equal proportions after both i.v. and oral doses (∼45%-48% each).
2.Potent sub-MIC effect of GSK1322322 and other peptide deformylase inhibitors on in vitro growth of Staphylococcus aureus.
Butler D;Chen D;O'Dwyer K;Lewandowski T;Aubart K;Zalacain M Antimicrob Agents Chemother. 2014;58(1):290-6. doi: 10.1128/AAC.01292-13. Epub 2013 Oct 28.
Peptide deformylase (PDF), a clinically unexploited antibacterial target, plays an essential role in protein maturation. PDF inhibitors, therefore, represent a new antibiotic class with a unique mode of action that provides an alternative therapy for the treatment of infections caused by drug-resistant pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). GSK1322322 is a novel PDF inhibitor that is in phase II clinical development for the treatment of lower respiratory tract and skin infections. We have discovered that PDF inhibitors can prevent S. aureus in vitro growth for up to 6 h at concentrations 8- to 32-fold below their MICs. This phenomenon seems specific to PDF inhibitors, as none of the antimicrobial agents with alternative mechanisms of action tested show such a potent and widespread effect. It also appears limited to S. aureus, as PDF inhibitors do not show such an inhibition of growth at sub-MIC levels in Streptococcus pneumoniae or Haemophilus influenzae. Analysis of the effect of GSK1322322 on the early growth of 100 randomly selected S. aureus strains showed that concentrations equal to or below 1/8× MIC inhibited growth of 91% of the strains tested for 6 h, while the corresponding amount of moxifloxacin or linezolid only affected the growth of 1% and 6% of strains, respectively.
3.Comparative analysis of the antibacterial activity of a novel peptide deformylase inhibitor, GSK1322322.
O'Dwyer K;Hackel M;Hightower S;Hoban D;Bouchillon S;Qin D;Aubart K;Zalacain M;Butler D Antimicrob Agents Chemother. 2013 May;57(5):2333-42. doi: 10.1128/AAC.02566-12. Epub 2013 Mar 11.
GSK1322322 is a novel peptide deformylase (PDF) inhibitor being developed for the intravenous and oral treatment of acute bacterial skin and skin structure infections and hospitalized patients with community-acquired pneumonia. The activity of GSK1322322 was tested against a global collection of clinical isolates of Haemophilus influenzae (n = 2,370), Moraxella catarrhalis (n = 115), Streptococcus pneumoniae (n = 947), Streptococcus pyogenes (n = 617), and Staphylococcus aureus (n = 940), including strains resistant to one or more marketed antibiotics. GSK1322322 had an MIC(90) of 1 μg/ml against M. catarrhalis and 4 μg/ml against H. influenzae, with 88.8% of β-lactamase-positive strains showing growth inhibition at that concentration. All S. pneumoniae strains were inhibited by ≤ 4 μg/ml of GSK1322322, with an MIC(90) of 2 μg/ml. Pre-existing resistance mechanisms did not affect its potency, as evidenced by the MIC(90) of 1 μg/ml for penicillin, levofloxacin, and macrolide-resistant S. pneumoniae. GSK1322322 was very potent against S. pyogenes strains, with an MIC(90) of 0.5 μg/ml, irrespective of their macrolide resistance phenotype. This PDF inhibitor was also active against S. aureus strains regardless of their susceptibility to methicillin, macrolides, or levofloxacin, with an MIC(90) of 4 μg/ml in all cases.
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