预制大环化合物库

Macrocycle Pre-Plated Set

产品编号： AN1400

Macrocycle Pre-Plated Set 包含25261个化合物。长期以来，药物化学家一直认为具有中型和大型环的化合物是一类独立的分子，这不仅是因为它们具有有趣的物理化学和生物学特性，还因为它们的合成具有挑战性。为了解决合成的可及性问题，ASINEX 利用有效的合成方法工具箱，包括固相支持合成、RCM、点击化学和扩环方法，精心制作了一个多样化的大环化合物库。

ASINEX 利用有效的合成方法工具箱，包括固相负载合成、RCM、点击化学和扩环，精心制作了一个多样化的大环化合物库。由此产生的骨架非常新颖，使我们能够生成种类繁多、与药物化学相关的大环结构。大环往往比传统的筛选分子大，这使它们成为浅表或扩展结合位点的靶点的完美发现工具。

同时，它们的独特特性基于受限的柔性和形成分子内氢键的能力，使设计方法能够有效优化水溶性和膜渗透性等特性。我们对许多大环化合物进行了水溶性和二甲基亚砜（DMSO）溶解性测试，在二甲基亚砜（DMSO）中的溶解度为 10 mM，在 PBS（pH 值为 7.4）中的溶解度为 50 µM，并进行了 PAMPA 渗透性测试。由于其构象灵活性受到限制，周围取代基的有利取向、许多大环有效地模拟了生物相关蛋白质的ɑ-螺旋或β-折叠拓扑结构。我们的大环化合物库为拟肽类物质提供了非常丰富的资源，非常适合研究具有挑战性的靶向类别，包括蛋白质-蛋白质相互作用、蛋白酶和抗菌剂等。

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Product Description

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.

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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
Empty	Vadadustat	TAK875	TAK-779	Tegobuvir	RN-1734	BMS-687453	AM211	FT011	BMS754807	AAI101	Empty
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
Empty	RPW-24	SRT1720 hydrochloride	INH6	SRT 2183	AMG208	Pentadecanoic acid	Apiopaeonoside	Pemirolast potassium	L-Anserine nitrate salt	Sodium Picosulfate	Empty
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
Empty	Lercanidipine	Cobicistat	1-Ethyl-2-benzimidazolinone	ROSIRIDIN	PF-AKT400	Benzyl alcohol	1-Methylnicotinamide chloride	MX69	CVT-10216	LCL161	Empty
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
Empty	Tirasemtiv	Roniacol	Rg3039	Z433927330	Desloratadine	CH5132799	5-Bromoindole	Smurf1-IN-A01	Halosulfuron-methyl	Piceatannol	Empty
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
Empty	ML346	SB 4	Daclatasvir	Daclatasvir dihydrochloride	NADPH (tetracyclohexanamine)	AZD8055	Vistusertib	PAβN dihydrochloride	HZ1157	Rotundine	Empty
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
Empty	Thiamet G	B-AP15	Silmitasertib	Levofloxacin	Pamicogrel	GSK369796 Dihydrochloride	2-Chloronaphthoquinone	TFAP	Tenovin3	Azvudine	Empty
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
Empty	Milnacipran hydrochloride	BW-A78U	Tenovin-6	DL-Normetanephrine hydrochloride	Triclocarban	CUDC101	Chlorpropham	Mestinon	Zacopride hydrochloride	PF04691502	Empty
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
Empty	L-Hyoscyamine	Noreugenin	ML-030	BC-1382	Gadolinium chloride	Vorolanib	VTP-27999 TFA	GSK0660	Lomerizine hydrochloride	8-CHLOROQUINAZOLIN-4(1H)-ONE	Empty

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