購物車 
-
地紅霉素
- names：
Dirithromycin
- CAS號：
62013-04-1
MDL Number： MFCD00865041 - MF(分子式)： C42H78N2O14 MW(分子量)： 835.07
- EINECS:624-080-7 Reaxys Number:
- Pubchem ID:6473883 Brand:BIOFOUNT
地紅霉素(62013-04-1,Dirithromycin,LY 237216)是大環(huán)內(nèi)酯類糖肽抗生素，能與細菌核糖體70S中的50S亞基相結(jié)合。
| 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 (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000154-500mg | 500mg | >98.0% | ￥ 633.75 | ￥ 633.75 | 2-3天 | ￥ 0.00 |
| 中文別名 | 地紅霉素(62013-04-1);地霉素;LY-237216；LY 237216；LY237216；地紅霉素; 抗生素AS-E 136;（9S）-9-脫氧-11-脫氧-9,11-（亞氨基（（1R）-2-（2-甲氧基乙氧基）亞乙基）氧基）紅霉素; |
| 英文別名 | Dirithromycin(62013-04-1);LY-237216; LY 237216; LY237216; Dirithromycin; Antibiotic AS-E 136;(9S)-9-deoxo-11-deoxy-9,11-(imino((1R)-2-(2-methoxyethoxy)ethylidene)oxy)erythromycin;dirithromycin;Dynabac;LY 237216;LY-237216;Nortron; |
| CAS號 | 62013-04-1 |
| Inchi | InChI=1S/C42H78N2O14/c1-15-29-42(10,49)37-24(4)32(43-30(56-37)21-52-17-16-50-13)22(2)19-40(8,48)36(58-39-33(45)28(44(11)12)18-23(3)53-39)25(5)34(26(6)38(47)55-29)57-31-20-41(9,51-14)35(46)27(7)54-31/h22-37,39,43,45-46,48-49H,15-21H2,1-14H3/t22-,23-,24+,25+,26-,27+,28+,29-,30-,31+,32+,33-,34+,35+,36-,37?,39+,40-,41-,42-/m1/s1 |
| InchiKey | WLOHNSSYAXHWNR-GETPLZSYSA-N |
| 分子式 Formula | C42H78N2O14 |
| 分子量 Molecular Weight | 835.07 |
| 溶解度Solubility | 生物體外In Vitro:Ethanol : ≥ 50 mg/mL(59.88 mM)DMSO溶解度33.33 mg/mL(39.91 mM;Need ultrasonic)*"≥" means soluble可溶, but saturation unknown溶解度未知. |
| 性狀 | 白色固體粉末,Power |
| 儲藏條件 Storage conditions | -20°C，3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月 |
地紅霉素(62013-04-1,Dirithromycin,LY 237216)毒性摘要：
The toxic symptoms following an overdose of a macrolide antibiotic may include nausea, vomiting, epigastric distress, and diarrhea.
地紅霉素(62013-04-1,Dirithromycin,LY 237216)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，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:地紅霉素試劑,地紅霉素合成,地紅霉素雜質(zhì),地紅霉素中間體,地紅霉素閃點,地紅霉素熔點,地紅霉素密度,地紅霉素溶解度,地紅霉素旋光度,地紅霉素購買,
| 產(chǎn)品說明 | 地紅霉素(62013-04-1,Dirithromycin,LY 237216)是一種大環(huán)內(nèi)酯類糖肽抗生素,通過與70S細菌核糖體的50S亞基結(jié)合來抑制肽的轉(zhuǎn)運. |
| Introduction | 地紅霉素(62013-04-1,Dirithromycin,LY 237216)is a macrolide glycopeptide antibiotic by binding to the 50S subunit of the 70S bacterial ribosome to inhibit the translocation of peptides. |
| Application1 | Dirithromycin與70S細菌核糖體的50S亞基結(jié)合，從而抑制了肽的轉(zhuǎn)運。 |
| Application2 | |
| Application3 |
地紅霉素(62013-04-1,Dirithromycin,LY 237216)藥理學：
1、地紅霉素（LY 237216）是一種大環(huán)內(nèi)酯糖肽類抗生素，通過與70S細菌核糖體的50S亞基結(jié)合來抑制肽的轉(zhuǎn)運。靶標：抗菌霉素是一種新的大環(huán)內(nèi)酯，其體外抗菌活性的光譜和程度類似于紅霉素。與紅霉素相比，地紅霉素具有更長的消除半衰期，可以每天給藥一次，并且在某些組織中還可以實現(xiàn)更高的細胞：細胞外濃度比和更高的濃度。多中心雙盲臨床試驗顯示，在治療呼吸道以及皮膚和軟組織的簡單細菌感染中，地霉素與紅霉素的療效相似。地霉素具有一些誘人的藥代動力學特性。與紅霉素相比，地霉素的消除半衰期長，因此可以每天給藥一次，并且組織濃度更高，更長。地紅霉素的活性譜，不良反應，臨床療效和細菌清除率可能與紅霉素相似。
2、地紅霉素是一種大環(huán)內(nèi)酯類糖肽抗生素，通過與70S細菌核糖體的50S亞基結(jié)合來抑制肽的轉(zhuǎn)運.Dirithromycin與70S細菌核糖體的50S亞基結(jié)合，從而抑制了肽的轉(zhuǎn)運。
3、地紅霉素是一種半合成的大環(huán)內(nèi)酯類抗生素前藥。地霉素在腸道吸收過程中通過水解轉(zhuǎn)化為具有微生物活性的紅霉素胺。乙丙胺與易感生物體70 S核糖體的50 S亞基結(jié)合，從而抑制細菌RNA依賴性蛋白的合成。這種抗生素用于治療由革蘭氏陽性微生物（包括金黃色葡萄球菌，肺炎鏈球菌和化膿性細菌），革蘭氏陰性微生物（包括流感嗜血桿菌，嗜肺乳桿菌）引起的呼吸道，皮膚和軟組織感染?？ㄋ暇头窝字гw。
4、 地紅霉素是由紅霉素衍生物（9S）- 紅霉素環(huán)胺與2-（2-甲氧基乙氧基）乙醛縮合產(chǎn)生的半縮醛。由于含半氨基的惡嗪環(huán)在酸性和堿性條件下均不穩(wěn)定，因此，紅霉素對（9S）-紅霉素具有更高的脂溶性前藥作用。以腸溶片的形式給藥，可保護其免受酸在胃中的水解，可用于治療易感生物引起的呼吸道，皮膚和軟組織感染。它具有前藥作用。
5、地紅霉素是一種大環(huán)內(nèi)酯類糖肽抗生素，用于治療許多不同類型的細菌感染，例如支氣管炎，肺炎，扁桃體炎，甚至皮膚感染。
1、地紅霉素（LY 237216）是一種大環(huán)內(nèi)酯糖肽類抗生素，通過與70S細菌核糖體的50S亞基結(jié)合來抑制肽的轉(zhuǎn)運。靶標：抗菌霉素是一種新的大環(huán)內(nèi)酯，其體外抗菌活性的光譜和程度類似于紅霉素。與紅霉素相比，地紅霉素具有更長的消除半衰期，可以每天給藥一次，并且在某些組織中還可以實現(xiàn)更高的細胞：細胞外濃度比和更高的濃度。多中心雙盲臨床試驗顯示，在治療呼吸道以及皮膚和軟組織的簡單細菌感染中，地霉素與紅霉素的療效相似。地霉素具有一些誘人的藥代動力學特性。與紅霉素相比，地霉素的消除半衰期長，因此可以每天給藥一次，并且組織濃度更高，更長。地紅霉素的活性譜，不良反應，臨床療效和細菌清除率可能與紅霉素相似。
2、地紅霉素是一種大環(huán)內(nèi)酯類糖肽抗生素，通過與70S細菌核糖體的50S亞基結(jié)合來抑制肽的轉(zhuǎn)運.Dirithromycin與70S細菌核糖體的50S亞基結(jié)合，從而抑制了肽的轉(zhuǎn)運。
3、地紅霉素是一種半合成的大環(huán)內(nèi)酯類抗生素前藥。地霉素在腸道吸收過程中通過水解轉(zhuǎn)化為具有微生物活性的紅霉素胺。乙丙胺與易感生物體70 S核糖體的50 S亞基結(jié)合，從而抑制細菌RNA依賴性蛋白的合成。這種抗生素用于治療由革蘭氏陽性微生物（包括金黃色葡萄球菌，肺炎鏈球菌和化膿性細菌），革蘭氏陰性微生物（包括流感嗜血桿菌，嗜肺乳桿菌）引起的呼吸道，皮膚和軟組織感染?？ㄋ暇头窝字гw。
4、 地紅霉素是由紅霉素衍生物（9S）- 紅霉素環(huán)胺與2-（2-甲氧基乙氧基）乙醛縮合產(chǎn)生的半縮醛。由于含半氨基的惡嗪環(huán)在酸性和堿性條件下均不穩(wěn)定，因此，紅霉素對（9S）-紅霉素具有更高的脂溶性前藥作用。以腸溶片的形式給藥，可保護其免受酸在胃中的水解，可用于治療易感生物引起的呼吸道，皮膚和軟組織感染。它具有前藥作用。
5、地紅霉素是一種大環(huán)內(nèi)酯類糖肽抗生素，用于治療許多不同類型的細菌感染，例如支氣管炎，肺炎，扁桃體炎，甚至皮膚感染。
| 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 | P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+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/護理 |
| 備注 | 實驗過程中防止吸入、食入，做好安全防護 |
地紅霉素(62013-04-1,Dirithromycin,LY 237216)危害標識：
| 象形圖 |  |
| 信號 | Warning |
| GHS危險說明 | Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory. |
| H317 (100%): May cause an allergic skin reaction [Warning Sensitization, Skin] | |
| 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, P280, P302+P352, P321, P333+P313, P363, and P501 |
| (The corresponding statement to each P-code can be found at the GHS Classification page.) |
| Brogden, R.N. and D.H. Peters, Dirithromycin. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic efficacy. Drugs, 1994. 48(4): p. 599-616. |
| Wintermeyer, S.M., S.M. Abdel-Rahman, and M.C. Nahata, Dirithromycin: a new macrolide. Ann Pharmacother, 1996. 30(10): p. 1141-9. |
| Sides, G.D., et al., Pharmacokinetics of dirithromycin. J Antimicrob Chemother, 1993. 31 Suppl C: p. 65-75. |
| Investigation of the in-vitro uptake, intraphagocytic biological activity and effects on neutrophil superoxide generation of dirithromycin compared with erythromycin PMID 1337069; The Journal of antim |
| The new macrolide antibiotics: azithromycin, clarithromycin, dirithromycin, and roxithromycin PMID 1318761; The Annals of pharmacotherapy 1992 Jan; 26(1):46-55 (Review Article) Name matches: azithromy |
地紅霉素(62013-04-1,Dirithromycin,LY 237216)參考文獻：
1.Quantitative determination of erythromycylamine in human plasma by liquid chromatography-mass spectrometry and its application in a bioequivalence study of dirithromycin.
Liu YQ1, Chen QY, Chen BM, Liu SG, Deng FL, Zhou P. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Mar 15;864(1-2):1-8. doi: 10.1016/j.jchromb.2007.12.021. Epub 2008 Jan 4.
A sensitive, rapid liquid chromatographic-electrospray ionization mass spectrometric method for determination of erythromycylamine in human plasma was developed and validated. Erythromycylamine in plasma (0.2 mL) was extracted with ethyl acetate, the organic phase was transferred to another clear 1.5 mL Eppendorf tube and evaporated to dryness under gentle nitrogen stream at 45 degrees C, and the residue was dissolved in 100 microL of mobile phase. The samples were separated using a Thermo Hypersil HyPURITY C18 reversed-phase column (150 mm x 2.1 mm I.D., 5 microm). A mobile phase containing 10 mM of ammonium acetate (pH = 6.4)-acetonitrile-methanol (50:10:40, v/v/v) was used isocratically eluting at a flow rate of 0.2 mL/min. Erythromycylamine and its internal standard (IS), midecamycin, were measured by electrospray ion source in positive selective ion monitoring mode. The method demonstrated that good linearity ranged from 4.5 to 720 ng/mL with r = 0.
2.Long-acting erythromycins: assessing their role in treating outpatient odontogenic infections.
Alexander RE1, Grogan DM. Tex Dent J. 2009 Apr;126(4):326-33.
Erythromycins have been part of our armamentarium against selected bacterial infections since they were discovered in 1952 and approved by the Food and Drug Administration (FDA) in 1964. In 1991, two newer, long-acting erythromycin analogues, azythromycin (brand name: Zithromax) and clarithromycin (brand name: Biaxin) were approved by the FDA. They were joined a few years later by a third long-acting form, dirithromycin (brand name: Dynabac).
3.Structural Correspondence of the Oriented Attachment Growth Mechanism of Crystals of the Pharmaceutical Dirithromycin.
Liang Z1, Wang Y1, Wang W1, Han X1, Chen JF1, Xue C1, Zhao H1. Langmuir. 2015 Dec 29;31(51):13802-12. doi: 10.1021/acs.langmuir.5b02901. Epub 2015 Dec 15.
The oriented attachment (OA) mechanism is promising for designing novel nanomaterials, yet an intensive understanding of the relationship between the crystal structure and attachment orientation is still lacking. In this work, we report layered hexagonal crystals of the pharmaceutical dirithromycin (DIR) containing multiple layers fabricated via a solvothermal method for a certain period of time at 40 °C. These elongated hexagonal crystals experience an OA that is preferentially on the face (001) of the initial crystals to assemble the final crystals into layered stacks. Through agreement with molecular modeling calculations, we predicted the final crystal growth morphology and confirmed the favored attachment surface based on the energy change ΔE following an OA event. These simulation results at the molecular level yielded good agreement with the crystal growth experiments. This study demonstrates the critical importance of combining experiments with a computational approach to understand the intrinsic molecular details of the OA growth mechanism of other compounds and to design nanomaterials with a desirable morphology and physical and chemical properties.
4.Epigallocatechin gallate as a modulator of Campylobacter resistance to macrolide antibiotics.
Kurin?i? M1, Klan?nik A, Smole Mo?ina S. Int J Antimicrob Agents. 2012 Nov;40(5):467-71. doi: 10.1016/j.ijantimicag.2012.07.015. Epub 2012 Sep 20.
Comprehensive therapeutic use of macrolides in humans and animals is important in the selection of macrolide-resistant Campylobacter isolates. This study shows high co-resistance to erythromycin, azithromycin, clarithromycin, dirithromycin and tylosin, with contributions from the 23S rRNA gene and drug efflux systems. The CmeABC efflux pump plays an important role in reduced macrolide susceptibility, accompanied by contributions from the CmeDEF efflux pump and potentially a third efflux pump. To improve clinical performance of licensed antibiotics and chemotherapeutic agents, it is important to understand the factors in Campylobacter that affect susceptibility to macrolide antibiotics. Using mutants that lack the functional genes coding for the CmeB and CmeF efflux pump proteins and the CmeR transcriptional repressor, we show that these efflux pumps are potential targets for the development of therapeutic strategies that use a combination of a macrolide with an efflux pump inhibitor (EPI) to restore macrolide efficacy.
1.Quantitative determination of erythromycylamine in human plasma by liquid chromatography-mass spectrometry and its application in a bioequivalence study of dirithromycin.
Liu YQ1, Chen QY, Chen BM, Liu SG, Deng FL, Zhou P. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Mar 15;864(1-2):1-8. doi: 10.1016/j.jchromb.2007.12.021. Epub 2008 Jan 4.
A sensitive, rapid liquid chromatographic-electrospray ionization mass spectrometric method for determination of erythromycylamine in human plasma was developed and validated. Erythromycylamine in plasma (0.2 mL) was extracted with ethyl acetate, the organic phase was transferred to another clear 1.5 mL Eppendorf tube and evaporated to dryness under gentle nitrogen stream at 45 degrees C, and the residue was dissolved in 100 microL of mobile phase. The samples were separated using a Thermo Hypersil HyPURITY C18 reversed-phase column (150 mm x 2.1 mm I.D., 5 microm). A mobile phase containing 10 mM of ammonium acetate (pH = 6.4)-acetonitrile-methanol (50:10:40, v/v/v) was used isocratically eluting at a flow rate of 0.2 mL/min. Erythromycylamine and its internal standard (IS), midecamycin, were measured by electrospray ion source in positive selective ion monitoring mode. The method demonstrated that good linearity ranged from 4.5 to 720 ng/mL with r = 0.
2.Long-acting erythromycins: assessing their role in treating outpatient odontogenic infections.
Alexander RE1, Grogan DM. Tex Dent J. 2009 Apr;126(4):326-33.
Erythromycins have been part of our armamentarium against selected bacterial infections since they were discovered in 1952 and approved by the Food and Drug Administration (FDA) in 1964. In 1991, two newer, long-acting erythromycin analogues, azythromycin (brand name: Zithromax) and clarithromycin (brand name: Biaxin) were approved by the FDA. They were joined a few years later by a third long-acting form, dirithromycin (brand name: Dynabac).
3.Structural Correspondence of the Oriented Attachment Growth Mechanism of Crystals of the Pharmaceutical Dirithromycin.
Liang Z1, Wang Y1, Wang W1, Han X1, Chen JF1, Xue C1, Zhao H1. Langmuir. 2015 Dec 29;31(51):13802-12. doi: 10.1021/acs.langmuir.5b02901. Epub 2015 Dec 15.
The oriented attachment (OA) mechanism is promising for designing novel nanomaterials, yet an intensive understanding of the relationship between the crystal structure and attachment orientation is still lacking. In this work, we report layered hexagonal crystals of the pharmaceutical dirithromycin (DIR) containing multiple layers fabricated via a solvothermal method for a certain period of time at 40 °C. These elongated hexagonal crystals experience an OA that is preferentially on the face (001) of the initial crystals to assemble the final crystals into layered stacks. Through agreement with molecular modeling calculations, we predicted the final crystal growth morphology and confirmed the favored attachment surface based on the energy change ΔE following an OA event. These simulation results at the molecular level yielded good agreement with the crystal growth experiments. This study demonstrates the critical importance of combining experiments with a computational approach to understand the intrinsic molecular details of the OA growth mechanism of other compounds and to design nanomaterials with a desirable morphology and physical and chemical properties.
4.Epigallocatechin gallate as a modulator of Campylobacter resistance to macrolide antibiotics.
Kurin?i? M1, Klan?nik A, Smole Mo?ina S. Int J Antimicrob Agents. 2012 Nov;40(5):467-71. doi: 10.1016/j.ijantimicag.2012.07.015. Epub 2012 Sep 20.
Comprehensive therapeutic use of macrolides in humans and animals is important in the selection of macrolide-resistant Campylobacter isolates. This study shows high co-resistance to erythromycin, azithromycin, clarithromycin, dirithromycin and tylosin, with contributions from the 23S rRNA gene and drug efflux systems. The CmeABC efflux pump plays an important role in reduced macrolide susceptibility, accompanied by contributions from the CmeDEF efflux pump and potentially a third efflux pump. To improve clinical performance of licensed antibiotics and chemotherapeutic agents, it is important to understand the factors in Campylobacter that affect susceptibility to macrolide antibiotics. Using mutants that lack the functional genes coding for the CmeB and CmeF efflux pump proteins and the CmeR transcriptional repressor, we show that these efflux pumps are potential targets for the development of therapeutic strategies that use a combination of a macrolide with an efflux pump inhibitor (EPI) to restore macrolide efficacy.
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