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            ジリスロマイシン

            ジリスロマイシン 化學構造式
            62013-04-1
            CAS番號.
            62013-04-1
            化學名:
            ジリスロマイシン
            別名:
            ジリスロマイシン;抗生物質AS-E-136;抗生物質AS-E136;(9S)-9-デオキソ-11-デオキシ-9,11-[イミノ[(R)-2-(2-メトキシエトキシ)エタン-1,1-ジイル]オキシ]エリスロマイシン;ジリトロマイシン
            英語化學名:
            Dirithromycin
            英語別名:
            Dynabac;ASE 136;Valodin;Noriclan;LY-237216;KT 237216;Dirithomycin;DIRITHROMYCIN;Dirythromycin;Diritromicina
            CBNumber:
            CB1337350
            化學式:
            C42H78N2O14
            分子量:
            835.07
            MOL File:
            62013-04-1.mol

            ジリスロマイシン 物理性質

            融點 :
            186-189° (dec) (Counter)
            沸點 :
            871.8±65.0 °C(Predicted)
            比重(密度) :
            1.19±0.1 g/cm3(Predicted)
            貯蔵溫度 :
            Sealed in dry,2-8°C
            溶解性:
            Very slightly soluble in water, very soluble in methanol and in methylene chloride
            外見 :
            solid
            酸解離定數(Pka):
            9.0 in 66% aq dimethyl fluoride
            色:
            white to off-white
            CAS データベース:
            62013-04-1(CAS DataBase Reference)
            安全性情報
            • リスクと安全性に関する聲明
            • 危険有害性情報のコード(GHS)
            主な危険性  Xn,Xi
            Rフレーズ  42/43-36/37/38
            Sフレーズ  36-26
            WGK Germany  3
            HSコード  29419000
            毒性 LD50 in mice (g/kg): >1 s.c.; >1 orally (Maier)
            絵表示(GHS)
            注意喚起語 Warning
            危険有害性情報
            コード 危険有害性情報 危険有害性クラス 區分 注意喚起語 シンボル P コード
            H317 アレルギー性皮膚反応を起こすおそれ 感作性、皮膚 1 警告 P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
            注意書き
            P280 保護手袋/保護衣/保護眼鏡/保護面を著用するこ と。

            ジリスロマイシン 価格 もっと(13)

            メーカー 製品番號 製品説明 CAS番號 包裝 価格 更新時間 購入
            富士フイルム和光純薬株式會社(wako) W01TRCD493000 ジリスロマイシン
            Dirithromycin
            62013-04-1 5mg ¥12500 2021-03-23 購入
            富士フイルム和光純薬株式會社(wako) W01TRCD493000 ジリスロマイシン
            Dirithromycin
            62013-04-1 10mg ¥13800 2021-03-23 購入
            東京化成工業 D5495 ジリスロマイシン >98.0%(HPLC)(N)
            Dirithromycin >98.0%(HPLC)(N)
            62013-04-1 1g ¥22000 2022-04-26 購入
            Sigma-Aldrich Japan D2880000 European Pharmacopoeia (EP) Reference Standard
            Dirithromycin European Pharmacopoeia (EP) Reference Standard
            62013-04-1 ¥35200 2021-03-23 購入
            Sigma-Aldrich Japan 1220700 United States Pharmacopeia (USP) Reference Standard
            Dirithromycin United States Pharmacopeia (USP) Reference Standard
            62013-04-1 200mg ¥55300 2021-03-23 購入

            ジリスロマイシン 化學特性,用途語,生産方法

            外観

            白色~ほとんど白色粉末~結晶

            効能

            抗生物質, タンパク質合成阻害薬

            説明

            Dirithromycin, an orally active oxazine derivative of erythromycin, is a secondgeneration macrolide antibiotic. It was first introduced in Spain for the treatment of respiratory tract, skin and soft tissue infections. It is safe and effective in treating acute bronchitis, acute bacterial exacerbation of chronic bronchitis, pneumonia, pharyngitis, and tonsillitis. Dirithromycin has been reported to have a similar antimicrobial spectrum and potency to erythromycin. However, compared to other macrolide antibiotics, dirithromycin has improved oral bioavailability, higher tissue permeability and longer duration of action. The once-daily therapy regiment is advantageous in terms of patient compliance and is a good alternative for patients who are unable to take penicillin.

            化學的特性

            white crystals

            使用

            Dirithromycin is a macrolide antibiotic pro-drug of 9S-erythromycylamine, a close analogue of erythromycin in which the 9-keto group is replaced with an amino group in the S-configuration. Although erythromycylamine overcomes the acid instability of erythromycin, it is poorly absorbed following oral administration. Dirithromycin is formed by reacting erythromycylamine with an aldehyde to form a Schiff base which undergoes cyclisation to an oxazine with the C11-alcohol. Dirithromycin provides higher tissue levels and prolonged in vivo half-life by slowly releasing erythromycylamine.

            定義

            ChEBI: The hemi-aminal resulting from the condensation of the erythromycin derivative (9S)-erythromycyclamine with 2-(2-methoxyethoxy)acetaldehyde. As the oxazine ring containing the hemi-aminal group is unstable under both acidic and alkaline co ditions, dirithromycin functions as a more lipid-soluble prodrug for (9S)-erythromycyclamine. Administered as enteric coated tablets to protect it from acid catalysed hydrolysis in the stomach, it is used to treat respiratory tract, skin, nd soft tissue infections caused by susceptible organisms.

            一般的な説明

            The incidence and severity of GI adverse effects associatedwith dirithromycin are similar to those seen with oralerythromycin. Preliminary studies indicate that dirithromycinand erythromycyclamine do not interact significantly with cytochromeP450 oxygenases. Thus, the likelihood of interferencein the oxidative metabolism of drugs such as phenytoin,theophylline, and cyclosporine by these enzymes may be lesswith dirithromycin than with erythromycin. Dirithromycin isrecommended as an alternative to erythromycin for the treatmentof bacterial infections of the upper and lower respiratorytracts, such as pharyngitis, tonsillitis, bronchitis, and pneumonia,and for bacterial infections of other soft tissues and theskin. The once-daily dosing schedule for dirithromycin is advantageousin terms of better patient compliance. Its place intherapy remains to be fully assessed.

            応用例(製薬)

            A prodrug of erythromycylamine, a semisynthetic erythromycin A derivative, formulated for oral administration. Activity against respiratory pathogens is generally poorer than that of erythromycin A.
            The long apparent elimination half-life (30–44 h) allows once-daily administration. Around 60–90% of a dose is converted to erythromycylamine within 35 min after intravenous administration. After oral administration of single doses of 500–1000 mg to healthy volunteers, the peak plasma concentrations ranged from 0.29 to 0.64 mg/L after 4–5 h. The absolute bioavailability after oral administration is about 10%. It achieves a higher concentration than erythromycin in some tissues. After a 500 mg single oral dose, the mean peak biliary concentration was 139 mg/L. Renal and non-renal clearance was lower in patients with biliary disease than in other patients or healthy volunteers.
            About 60–80% of an oral dose and over 80% of an intravenous dose are eliminated in the feces, predominantly as erythromycylamine. Dosage adjustments do not appear necessary in patients with mild or moderate hepatic, biliary or renal impairment. Negligible amounts of the drug are removed during hemodialysis.
            Adverse events are similar to those found with other macrolides. Gastrointestinal events are most common; around 5% of patients experience abdominal pain, diarrhea or nausea.
            It has been used in community-acquired infections of the respiratory tract and skin and soft-tissue infections. It is no longer widely available.

            ジリスロマイシン 上流と下流の製品情報

            原材料

            準備製品


            ジリスロマイシン 生産企業

            Global( 230)Suppliers
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            Henan Tianfu Chemical Co.,Ltd.
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            info@tianfuchem.com China 22021 55
            Guangzhou PI PI Biotech Inc
            +8618371201331
            87478684@qq.com China 3640 55
            career henan chemical co
            +86-0371-86658258
            sales@coreychem.com China 29959 58
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            Hubei Jusheng Technology Co.,Ltd.
            86-18871470254
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            Hebei Guanlang Biotechnology Co., Ltd.
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            alice@crovellbio.com China 5953 58
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            CONIER CHEM AND PHARMA LIMITED
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            sales@conier.com China 47501 58
            Shaanxi Dideu Medichem Co. Ltd
            +86-29-87569265 18612256290
            Service@dideu.com China 3993 58

            62013-04-1(ジリスロマイシン)キーワード:


            • 62013-04-1
            • [9S(R)]-9-Deoxo-11-deoxy-9,11-[imino[2-(2-methoxyethoxy)ethylidene]oxy]erythromycin
            • Antibiotic AS-E 136
            • ASE 136
            • Dirythromycin
            • LY-237216
            • DIRITHROMYCIN
            • [9S(R)]-9-DEOXO-11-DEOXY-9,11-[IMINO[2-(2-METHOXY)ETHYLIDENE]OXY]ERTHROMYCIN
            • [9s(r)]-9-deoxo-11-deoxy-9,11-[imino[2-(2-methoxy)ethylidene]oxy]erthromycin,ly-237216
            • Dirithomycin
            • 9-(4-Dimethylamino-3-hydroxy-6-methyl-oxan-2-yl)oxy-3-ethyl-2,10-dihydroxy-7-(5-hydroxy-4-methoxy-4,6-dimethyl-oxan-2-yl)oxy-15-(2-methoxyethoxymethyl)-2,6,8,10,12,17-hexamethyl-4,16-dioxa-14-azabicyclo[11.3.1]heptadecan-5-one
            • Dynabac
            • KT 237216
            • Noriclan
            • Valodin
            • 4,16-Dioxa-14-azabicyclo[11.3.1]heptadecan-5-one, 7-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-3-ethyl-2,10-dihydroxy-15-[(2-methoxyethoxy)methyl]-2,6,8,10,12,17-hexamethyl-9-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-, (1R,2R,3R,6R,7S,8S,9R,10R,12R,13S,15R,17S)-
            • [9S]-9-Deoxo-11-deoxy-9,11-[imino[2-(2methoxyethoxy)ethylidene]oxy]erythromycin
            • (2R,3R,6R,7S,8S,9R,10R,12R,13S,15R,17S)-9-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyl-oxan-2-yl]oxy-3-ethyl-2,10-dihydroxy-7-[(2S,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyl-oxan-2-yl]oxy-15-(2-methoxyethoxymethyl)-2,6,8,10,12,17-hexamethyl-4,16-dioxa-14-azabicyclo[11.3.1]heptadecan-5-one
            • (9S)-9-Deoxo-11-deoxy-9,11-(imino((1R)-2-(2-methoxyethoxy)ethylidene)oxy)erythromycin
            • (9S)-9-Deoxo-11-deoxy-9,11-[imino[(R)-2-(2-methoxyethoxy)ethane-1,1-diyl]oxy]erythromycin
            • Dirithromycin (200 mg)
            • DirithroMycin/LY-237216
            • 16S-Dierythromycin Isomer
            • Dirithromycin Impurit Ⅱ: [9S(R)]-9-Deoxo-11-deoxy-9,11-[imino[2-(2-methoxyethoxy)ethylidene]oxy]erythromycin(Dirithromycin)
            • (1S,2R,4R,5R,6S,7S,8R,11R,12R,13R,15R,17S)-5-[[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyl-2-oxanyl]oxy]-11-ethyl-4,12-dihydroxy-7-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyl-2-oxanyl]oxy]
            • Dirithromycin CRS
            • Dirithromycine
            • Dirithromycinum
            • Diritromicina
            • 4,16-Dioxa-14-azabicyclo[11.3.1]heptadecan-5-one, 7-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-3-ethyl-2,10-dihydroxy-15-[(2-methoxyethoxy)methyl]-2,6,8,10,12,17-hexamethyl-9-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-, (1R,2R,3R,6R,7S,8S,9R,10R,12R,13S,15R,1...
            • (1R,2R,3R,6R,7S,8S,9R,10R,12R,13S,15R,17S)-9-(((2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-3-ethyl-2,10-dihydroxy-7-(((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-15-((2-methoxyethoxy)methyl)-2,6,8,10,12,17-hexamethyl-4,16-dioxa-14-azabicyclo[11.3.1]heptadecan-5-one
            • ジリスロマイシン
            • 抗生物質AS-E-136
            • 抗生物質AS-E136
            • (9S)-9-デオキソ-11-デオキシ-9,11-[イミノ[(R)-2-(2-メトキシエトキシ)エタン-1,1-ジイル]オキシ]エリスロマイシン
            • ジリトロマイシン
            • マクロライド系抗生物質
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