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an_macrocycles_library
/library/an_macrocycles_library
大环化合物库AN
AN Macrocycles Library
产品编号: AN3300

为了解决合成可行性的问题,ASINEX 利用固相负载合成、RCM、点击化学和环扩展等有效的合成方法,精心设计了一个多样化的大环化合物库。该库包含10091个化合物。长期以来,药物化学家一直将中型和大型环的化合物视为一类独特的分子,这不仅因为它们具有有趣的物理化学和生物学特性,还因为它们在合成方面具有挑战性。

ASINEX 通过使用固相负载合成、RCM、点击化学和环扩展等有效的合成方法,构建了一个多样化的大环化合物库。所得到的分子结构是全新的,使我们能够生成非常多样化的与药物化学相关的大环骨架。大环化合物往往比传统的筛选分子要大,这使它们成为探索具有浅表面或延伸结合位点的靶点的完美工具。同时,它们具有独特的性质,如有限的柔性和形成分子内氢键的能力,使得设计方法能够有效地优化其水溶性和膜渗透性等性质。我们的许多大环化合物已经进行了水和DMSO 溶解度的测试,DMSO 溶解度的截断值为10 mM,PBS(pH 7.4)中的溶解度截断值为50 µM,随后进行了PAMPA 渗透性测定。由于其受限的构象柔性以及周边取代基的有利取向,许多大环化合物能够有效地模拟与生物相关的蛋白质的α-螺旋或β-发夹拓扑结构。我们的大环化合物库提供了丰富的类肽模拟物,并且非常适合研究包括蛋白质相互作用、蛋白酶和抗菌剂等具有挑战性的靶点类别。

陶术生物的所有产品和服务仅用于科学研究,我们不为任何个人用途提供产品和服务。
产品规格

ASINEX has elaborated a library of diverse macrocycles using an effective toolbox of synthetic methods including solid phase-supported synthesis, RCM, click-chemistry, and ring expansion. The resulting scaffolds are novel and have allowed us to generate tremendously diverse, Medchem relevant, macrocyclic frameworks. Macrocycles tend to be larger than traditional screening molecules which makes them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such as aqueous solubility and membrane permeability. Many of our macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay. Due to their restricted conformational flexibility accompanied by a favorable orientation of peripheral substituents, many macrocycles effectively mimic the ɑ-helical or β-hairpin topology of biologically relevant proteins. Our Macrocyclic Library provides a very rich source of peptidomimetics and is ideal for probing challenging target classes including protein-protein interactions, proteases, and antibacterials.

化合物库定制
我们的化合物库可以灵活定制!了解更多
化合物库咨询
化合物库组成
化合物库信息示例
Empty 1000025-07-9 1000413-72-8 229005-80-5 1000787-75-6 946387-07-1 1000998-59-3 1175526-27-8 1001288-58-9 1001350-96-4 1001404-83-6 Empty
Vadadustat TAK875 TAK-779 Tegobuvir RN-1734 BMS-687453 AM211 FT011 BMS754807 AAI101
Empty 1001625-82-6 1001645-58-4 1001753-24-7 1001908-89-9 1002304-34-8 1002-84-2 100291-86-9 100299-08-9 10030-52-1 10040-45-6 Empty
RPW-24 SRT1720 hydrochloride INH6 SRT 2183 AMG208 Pentadecanoic acid Apiopaeonoside Pemirolast potassium L-Anserine nitrate salt Sodium Picosulfate
Empty 100427-26-7 1004316-88-4 10045-45-1 100462-37-1 1004990-28-6 100-51-6 1005-24-9 1005264-47-0 1005334-57-5 1005342-46-0 Empty
Lercanidipine Cobicistat 1-Ethyl-2-benzimidazolinone ROSIRIDIN PF-AKT400 Benzyl alcohol 1-Methylnicotinamide chloride MX69 CVT-10216 LCL161
Empty 1005491-05-3 100-55-0 1005504-62-0 1005883-72-6 100643-71-8 1007207-67-1 10075-50-0 1007647-73-5 100784-20-1 10083-24-6 Empty
Tirasemtiv Roniacol Rg3039 Z433927330 Desloratadine CH5132799 5-Bromoindole Smurf1-IN-A01 Halosulfuron-methyl Piceatannol
Empty 100872-83-1 100874-08-6 1009119-64-5 1009119-65-6 100929-71-3 1009298-09-2 1009298-59-2 100929-99-5 1009734-33-1 10097-84-4 Empty
ML346 SB 4 Daclatasvir Daclatasvir dihydrochloride NADPH (tetracyclohexanamine) AZD8055 Vistusertib PAβN dihydrochloride HZ1157 Rotundine
Empty 1009816-48-1 1009817-63-3 1009820-21-6 100986-85-4 101001-34-7 1010411-21-8 1010-60-2 1011244-68-0 1011301-27-1 1011529-10-4 Empty
Thiamet G B-AP15 Silmitasertib Levofloxacin Pamicogrel GSK369796 Dihydrochloride 2-Chloronaphthoquinone TFAP Tenovin3 Azvudine
Empty 101152-94-7 101155-02-6 1011557-82-6 1011-74-1 101-20-2 1012054-59-9 101-21-3 101-26-8 101303-98-4 1013101-36-4 Empty
Milnacipran hydrochloride BW-A78U Tenovin-6 DL-Normetanephrine hydrochloride Triclocarban CUDC101 Chlorpropham Mestinon Zacopride hydrochloride PF04691502
Empty 101-31-5 1013-69-0 1013750-77-0 1013753-99-5 10138-52-0 1013920-15-4 1013937-63-7 1014691-61-2 101477-54-7 101494-95-5 Empty
L-Hyoscyamine Noreugenin ML-030 BC-1382 Gadolinium chloride Vorolanib VTP-27999 TFA GSK0660 Lomerizine hydrochloride 8-CHLOROQUINAZOLIN-4(1H)-ONE
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