购物车 
-
拉诺培登
- names：
Lanopepden
- CAS号：
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
拉诺培登(1152107-25-9,Lanopepden,GSK 1322322)是一种肽去甲酰胺酶抑制剂，GSK 1322322可抑制金黄色葡萄球菌。GSK 1322322抑制ATCC 29213和ATCC 25923甲苯，MIC都为1 mg / L。
| 货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
|---|---|---|---|---|---|---|---|---|
| YZM000166-1mg | 1mg | >97% | ¥ 3412.50 | ¥ 3412.50 | 2-3天 | ¥ 0.00 |
| 中文别名 | 拉诺培登(1152107-25-9);拉诺培登 ;N-[（2R）-2-（环戊基甲基）-3-（2- {5-氟-6-[（9aS）-六氢吡嗪并[2,1-c] [1,4]恶嗪-8（1H）-酰基]-2-甲基嘧啶-4-基}肼-1-基）-3-氧丙基]-N-羟基甲酰胺，GSK-1322322，GSK-322； |
| 英文别名 | 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号 | 1152107-25-9 |
| SMILES | FC1=C(N2CCN(CCOC3)[C@@]3([H])C2)N=C(C)N=C1NNC([C@H](CC4CCCC4)CN(C=O)O)=O |
| 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 |
| 闪点 FP | |
| 熔点 Melting point | No data available |
| 沸点 Boiling point | |
| Polarizability极化度 | 48.5±0.5 10-24cm3 |
| 密度 Density | 1.4±0.1 g/cm3 |
| 蒸汽压 Vapor Pressure | |
| 溶解度Solubility | |
| 性状 | 固体粉末,Power |
| 储藏条件 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 |
拉诺培登(1152107-25-9,Lanopepden,GSK 1322322)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:拉诺培登试剂,拉诺培登杂质,拉诺培登合成,拉诺培登密度,拉诺培登溶解度,拉诺培登旋光度,拉诺培登闪点,拉诺培登熔点,拉诺培登购买,拉诺培登MSDS,
| 产品说明 | 拉诺培登(1152107-25-9,Lanopepden,GSK 1322322)是一种肽去甲酰基酶抑制剂,对金黄色葡萄球菌菌株具有活性 |
| Introduction | 拉诺培登(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 | 拉诺培登(1152107-25-9,Lanopepden,GSK 1322322)对ATCC 29213和ATCC 25923菌株的MIC分别为1和1 mg / L，已用于研究治疗肺炎，感染，细菌，皮肤病，感染和皮肤感染，细菌的试验中。 |
| Application2 | |
| Application3 |
拉诺培登(1152107-25-9,Lanopepden,GSK 1322322)药理学：
1、该活性分子是选择性肽去甲酰基酶抑制剂。在体外具有良好的抗菌活性。Lanopepden的抗菌谱包括肺炎链球菌，流感嗜血杆菌，化脓性链球菌和金黄色葡萄球菌，这表明在29个月的24小时内，在4×MIC下CFU / ml的数量降低了≥3-log（10）。测试了33个菌株。它也可以用于治疗由耐药菌引起的传染病。2015年1月1日，葛兰素史克（GlaxoSmithKline）撤回了美国细菌感染的I期试验。2015年1月26日，葛兰素史克（GlaxoSmithKline）撤回了美国健康志愿者的第一阶段药代动力学/药效学试验。
2、Lanopepden（GSK 1322322）是一种肽去甲酰基酶抑制剂，对金黄色葡萄球菌菌株具有活性，对ATCC 29213和ATCC 25923菌株的MIC分别为1和1 mg / L。
1、该活性分子是选择性肽去甲酰基酶抑制剂。在体外具有良好的抗菌活性。Lanopepden的抗菌谱包括肺炎链球菌，流感嗜血杆菌，化脓性链球菌和金黄色葡萄球菌，这表明在29个月的24小时内，在4×MIC下CFU / ml的数量降低了≥3-log（10）。测试了33个菌株。它也可以用于治疗由耐药菌引起的传染病。2015年1月1日，葛兰素史克（GlaxoSmithKline）撤回了美国细菌感染的I期试验。2015年1月26日，葛兰素史克（GlaxoSmithKline）撤回了美国健康志愿者的第一阶段药代动力学/药效学试验。
2、Lanopepden（GSK 1322322）是一种肽去甲酰基酶抑制剂，对金黄色葡萄球菌菌株具有活性，对ATCC 29213和ATCC 25923菌株的MIC分别为1和1 mg / L。
| 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 |
拉诺培登(1152107-25-9,Lanopepden,GSK 1322322)危害标识：
| 象形图 |  |
| 信号 | Warning |
| GHS危险说明 | 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] | |
| 防范说明代码 | 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- |
拉诺培登(1152107-25-9,Lanopepden,GSK 1322322)参考文献：
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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