CAS: 844439-96-9; 16-[[(1S)-4-[[(5S)-5-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[2-[[(1R,6R,12S,15S,18S,21S,24S,27S,30S,33S,36S,39S,42R,47R,50S,53S,56S,59S,62S,65S,68S,71S,74R,77S,80S,83S,88R)-88-[[(2S)-5-Amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[(2-Aminoacetyl)Amino]-3-Methylpentanoyl]Amino]-3-Methylbutanoyl]Amino]-4-Carboxybutanoyl]Amino]-5-Oxopentanoyl]Amino]-6-[[(2S)-2-[[(2S)-2-[[(2S)-5-Amino-2-[[(2S)-4-Amino-2-[[(2S)-2-[[(2S)-2-Amino-3-Phenylpropanoyl]Amino]-3-Methylbutanoyl]Amino]-4-Oxobutanoyl]Amino]-5-Oxopentanoyl]Amino]-3-(1H-Imidazol-4-yl)Propanoyl]Amino]-4-Methylpentanoyl]Amino]-47-[[(1S)-3-Amino-1-Carboxy-3-Oxopropyl]Carbamoyl]-53-(2-Amino-2-Oxoethyl)-62-(3-Amino-3-Oxopropyl)-77-[(2S)-Butan-2-Yl]-24,56-Bis(2-Carboxyethyl)-83-[(1R)-1-Hydroxyethyl]-12,71,80-Tris(Hydroxymethyl)-33,50,65-Tris[(4-Hydroxyphenyl)Methyl]-15-(1H-Imidazol-4-Ylmethyl)-27-Methyl-18,30,36,59,68-Pentakis(2-Methylpropyl)-7,10,13,16,19,22,25,28,31,34,37,40,49,52,55,58,61,64,67,70,73,76,79,82,85,87-Hexacosaoxo-21,39-Di(Propan-2-yl)-3,4,44,45,90,91-Hexathia-8,11,14,17,20,23,26,29,32,35,38,41,48,51,54,57,60,63,66,69,72,75,78,81,84,86-Hexacosazabicyclo[72.11.7]Dononacontane-42-Carbonyl]Amino]Acetyl]Amino]-4-Carboxybutanoyl]Amino]-5-Carbamimidamidopentanoyl]Amino]Acetyl]Amino]-3-Phenylpropanoyl]Amino]-3-Phenylpropanoyl]Amino]-3-(4-Hydroxyphenyl)Propanoyl]Amino]-3-Hydroxybutanoyl]Pyrrolidine-2-Carbonyl]Amino]-5-Carboxypentyl]Amino]-1-Carboxy-4-Oxobutyl]Amino]-16-Oxohexadecanoic Acid

该化合物是一种长期作用的胰岛素类比,主要用于糖尿病的治疗,其特点是独特的分子结构,其中包括允许与普通胰岛素相比长期行动的一种改变,与普通胰岛素相比,允许长期行动.这一修改涉及增加脂肪酸链,使多氧素在亚皮层组织中形成,导致缓慢和稳定地释放到血液中.胰岛脱底醇具有相对平坦的药用植物遗传学特征,有助于最大限度地降低低血糖的风险,并允许灵活施药时间表.通常通过亚乳注射进行,并与其他抗糖尿病药物结合使用.行动的开始是渐进的,效果长达42小时,适合一次服用.与其他胰岛素疗法一样,监测血糖水平对于确保有效的血糖控制,同时最大限度地减少可能的副作用至关重要.

英文名称16-[[(1S)-4-[[(5S)-5-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[2-[[(1R,6R,12S,15S,18S,21S,24S,27S,30S,33S,36S,39S,42R,47R,50S,53S,56S,59S,62S,65S,68S,71S,74R,77S,80S,83S,88R)-88-[[(2S)-5-Amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[(2-Aminoacetyl)Amino]-3-Methylpentanoyl]Amino]-3-Methylbutanoyl]Amino]-4-Carboxybutanoyl]Amino]-5-Oxopentanoyl]Amino]-6-[[(2S)-2-[[(2S)-2-[[(2S)-5-Amino-2-[[(2S)-4-Amino-2-[[(2S)-2-[[(2S)-2-Amino-3-Phenylpropanoyl]Amino]-3-Methylbutanoyl]Amino]-4-Oxobutanoyl]Amino]-5-Oxopentanoyl]Amino]-3-(1H-Imidazol-4-yl)Propanoyl]Amino]-4-Methylpentanoyl]Amino]-47-[[(1S)-3-Amino-1-Carboxy-3-Oxopropyl]Carbamoyl]-53-(2-Amino-2-Oxoethyl)-62-(3-Amino-3-Oxopropyl)-77-[(2S)-Butan-2-Yl]-24,56-Bis(2-Carboxyethyl)-83-[(1R)-1-Hydroxyethyl]-12,71,80-Tris(Hydroxymethyl)-33,50,65-Tris[(4-Hydroxyphenyl)Methyl]-15-(1H-Imidazol-4-Ylmethyl)-27-Methyl-18,30,36,59,68-Pentakis(2-Methylpropyl)-7,10,13,16,19,22,25,28,31,34,37,40,49,52,55,58,61,64,67,70,73,76,79,82,85,87-Hexacosaoxo-21,39-Di(Propan-2-yl)-3,4,44,45,90,91-Hexathia-8,11,14,17,20,23,26,29,32,35,38,41,48,51,54,57,60,63,66,69,72,75,78,81,84,86-Hexacosazabicyclo[72.11.7]Dononacontane-42-Carbonyl]Amino]Acetyl]Amino]-4-Carboxybutanoyl]Amino]-5-Carbamimidamidopentanoyl]Amino]Acetyl]Amino]-3-Phenylpropanoyl]Amino]-3-Phenylpropanoyl]Amino]-3-(4-Hydroxyphenyl)Propanoyl]Amino]-3-Hydroxybutanoyl]Pyrrolidine-2-Carbonyl]Amino]-5-Carboxypentyl]Amino]-1-Carboxy-4-Oxobutyl]Amino]-16-Oxohexadecanoic Acid
中文名称德谷胰岛素
CAS编号844439-96-9
分子式:C274H411N65O81S6分子量:6103.97204
产品CID: 1832704
产品分类原料药 → 激素及调节内分泌功能类药 → 胰腺激素及其它调节血糖药

相似结构搜索
InChIKey: FYZPCMFQCNBYCY-WIWKJPBBSA-N
FYZPCMFQCNBYCY-WIWKJPBBSA-N
计算化学: 氢键受体数92.0氢键供体数79.0可旋转键数197.0

MSDS等安全信息

合成工艺路线路线简述

海关参考信息

2902600000-乙苯
2905122000-异丙醇
2912110000-甲醛
2912120000-乙醛
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专利信息

专利号:AU-2020409711-A1
优先权日:2019-12-20
标题 :Synthesis of lactone derivatives and their use in the modification of proteins

专利号:BR-112014026077-B1
优先权日:2012-04-20
标题 :METHOD OF SOLID PHASE SYNTHESIS OF A PROTECTED, PARTIALLY PROTECTED OR UNPROTECTED INSULIN B CHAIN OR AN INSULIN B CHAIN DERIVATIVE, AND METHOD FOR PREPARING AN INSULIN B CHAIN PEPTIDE

专利号:EP-4076533-A1
优先权日:2019-12-20
标题:Synthesis of lactone derivatives and their use in the modification of proteins

专利号:WO-2013156977-A1
优先权日:2012-04-20
标题 :Solid phase peptide synthesis of insulin using side chain anchored lysine

专利号:CA-3164962-A1
优先权日:2019-12-20
标题 :Synthesis of lactone derivatives and their use in the modification of proteins

专利号:US-2016031962-A1
优先权日:2012-04-20
标题 :Solid phase peptide synthesis of insulin using side chain achored lysine

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合成参考文献

参考文献:10.1007/s10620-015-3907-2
摘要:García-Compeán D, González-González JA, Lavalle-González FJ, González-Moreno EI, Villarreal-Pérez JZ, Maldonado-Garza HJ. Current Concepts in Diabetes Mellitus and Chronic Liver Disease: Clinical Outcomes, Hepatitis C Virus Association, and Therapy. Digestive Diseases and Sciences. 2015 Oct 13;61(2):371–80. doi: 10.1007/s10620-015-3907-2.
参考文献:10.1007/s13300-018-0430-4
摘要:Pollock RF, Valentine WJ, Marso SP, Gundgaard J, Hallén N, Hansen LL, Tutkunkardas D, Buse JB, On behalf of the DEVOTE Study Group. DEVOTE 5: Evaluating the Short-Term Cost-Utility of Insulin Degludec Versus Insulin Glargine U100 in Basal–Bolus Regimens for Type 2 Diabetes in the UK. Diabetes Therapy. 2018 Apr 30;9(3):1217–32. doi: 10.1007/s13300-018-0430-4.
参考文献:10.1186/s12955-018-0883-1
摘要:Weatherall J, Polonsky WH, Lanar S, Knoble N, Håkan-Bloch J, Constam E, Philis-Tsimikas A, Marrel A. When insulin degludec enhances quality of life in patients with type 2 diabetes: a qualitative investigation. Health and Quality of Life Outcomes. 2018 May 03;16(1):87. doi: 10.1186/s12955-018-0883-1.
参考文献:10.1208/s12249-018-1032-1
摘要:Nie L, Hu M, Yan X, Guo T, Wang H, Zhang S, Qu H. Optimization of a Coupling Process for Insulin Degludec According to a Quality by Design (QbD) Paradigm. AAPS PharmSciTech. 2018 Jul;19(5):2185–94. doi: 10.1208/s12249-018-1032-1.
参考文献:10.1007/s40258-019-00494-3
摘要:Pollock RF, Valentine WJ, Marso SP, Andersen A, Gundgaard J, Hallén N, Tutkunkardas D, Magnuson EA, Buse JB; DEVOTE study group. Long-term Cost-effectiveness of Insulin Degludec Versus Insulin Glargine U100 in the UK: Evidence from the Basal-bolus Subgroup of the DEVOTE Trial (DEVOTE 16). Appl Health Econ Health Policy. 2019 Oct;17(5):615–27.