AZ084

≥99%

CAS编号: 929300-19-6
分子式: \n C₂₆H₃₄N₄O₂
分子量: 434.57
PubChem编号: 16065569

有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

货号 (SKU)	包装规格	是否现货
A646309-1mg	1mg	期货
A646309-5mg	5mg	期货
A646309-10mg	10mg	期货
A646309-50mg	50mg	期货

查看相关系列

CCR (85) GPCR/G Protein (3182) Immunology/Inflammation (1941)

Skip to the end of the images gallery

Skip to the beginning of the images gallery

基本描述

规格或纯度	≥99%
英文名称	AZ084
生化机理	AZ084 是一种强效、选择性、异位和口服活性 CCR8 异位拮抗剂，其 K i 为 0.9 nM。具有治疗哮喘的潜力。AZ084 可抑制免疫耐受的转移前生态位（PMN）的形成和肿瘤细胞的转移。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a K i of 0.9 nM. Has potential to treat asthma AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer In Vitro AZ084 (5 μg/mL; single daily for 4 days) suppresses proportion of Tregs and reduces T cells that expresses CCR8 (co-cultured in vitro with LLC-exo MPF CM). ?\nAZ084 (0-10 μM) inhibits AML, DC and T cells with IC 50 s of 1.3, 4.6 and 5.7 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Splenic T cells Concentration: 5 μg/mL (single daily) Incubation Time: 4 days Result: Reversed the increased proportion of Tregs among the CD4+ T cells co-cultured in vitro with LLC-exo MPF CM. Reduced T cells that expressed CCR8 (cultured in vitro with by LLC-exo MPF CM). Cell Viability AssayCell Line: AML, DC and T cells Concentration: 0-10 µM Incubation Time: Result: Showed high potency with pronounced dose-response dependent inhibition of chemotaxis with an IC 50 of 1.3 nM in AML cells. In Vivo AZ084 (5 mg/kg; i.p.; every third day for 9 or 21 days) restrains the formation of the immunologically tolerant PMN and tumor cells metastasis in lung by downregulating Treg differentiation . ?\nAZ084 (434.57-869.14 mg/kg; i.v.; single) shows a bioavailability >70% in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 J mice (subcutaneous LLC tumor model) . Dosage: 5 mg/kg Administration: Intraperitoneal injection, every third day for 9 or 21 days. Result: Inhibited Treg differentiation and tumor cell colonization of the lungs and reduced the number of CD4+Foxp3+ Tregs in the lungs of LLC-exo pre-injected mice (every third day for 9 days). Inhibited the LLC-exo-induced LLC cell seeding in lung and also significantly reduced Treg accumulation in LLC-exo stimulated mouse lungs(every third day for 21 days). Animal Model: Female Balb/C mice, male Wistar rats and female Beagle dogs. Dosage: 434.57-869.14 mg/kg (in 0.9% NaCl) Administration: Intravenous injection, single. Result: 1.19 Pharmacokinetic Parameters of AZ084 in Female Balb/C mice, male Wistar rats and female Beagle dogs. IV (434.57-869.14 mg/kg) Dog plasma protein binding (% free) 45.7 Mu plasma protein binding (% free) 55.6 Hu plasma protein binding (% free) 31.0 Rat plasma protein binding (% free) 47.0 Rat HW plasma PK CL (mL/min/kg) 15.0 Rat HW plasma PK V ss (L/kg) 6.0 Rat HW plasma PK T 1/2 (h) 5.4 Rat HW plasma PK C max (µM) 0.5 Rat HW plasma PK bioavailability (%) 68.0 Form:Solid IC50& Target:CCR8 0.9 nM (Ki)

关联靶点（人）

CCR8 Tchem CC 趋化因子受体 8 型(C-C chemokine receptor type 8) (1 活性数据)

点击查看靶蛋白信息： CCR8

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

KCNH2 Tclin HERG (29587 活性数据)

点击查看靶蛋白信息： KCNH2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	小分子
IUPAC Name	(5-aminopyridin-2-yl)-[9-[(2,2-dimethyl-3H-1-benzofuran-4-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone
INCHI	InChI=1S/C26H34N4O2/c1-25(2)16-21-19(4-3-5-23(21)32-25)18-29-12-8-26(9-13-29)10-14-30(15-11-26)24(31)22-7-6-20(27)17-28-22/h3-7,17H,8-16,18,27H2,1-2H3
InChi Key	WIGFMKMFRGRSDE-UHFFFAOYSA-N
Canonical SMILES	CC1(CC2=C(C=CC=C2O1)CN3CCC4(CC3)CCN(CC4)C(=O)C5=NC=C(C=C5)N)C
Isomeric SMILES	CC1(CC2=C(C=CC=C2O1)CN3CCC4(CC3)CCN(CC4)C(=O)C5=NC=C(C=C5)N)C
PubChem CID	16065569
分子量	434.57

化学和物理性质

溶解性	DMSO : 250 mg/mL (575.28 mM; Need ultrasonic)
分子量	434.600 g/mol
XLogP3	3.200
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	5
可旋转键计数Rotatable Bond Count	3
精确质量Exact Mass	434.268 Da
单同位素质量Monoisotopic Mass	434.268 Da
拓扑极表面积Topological Polar Surface Area	71.700 Å²
重原子数Heavy Atom Count	32
形式电荷Formal Charge	0
复杂度Complexity	665.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

安全和危险性（GHS）

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

输入批号以搜索分析图谱:

溶液计算器

摩尔浓度计算器

计算溶液所需的质量、体积或浓度。

质量

浓度

体积

分子量

g/mol

稀释计算器

计算配制储备溶液所需的稀释度。

浓度1（C1）

体积 1 (V1)

浓度 2 (C2)

体积 2 (V2)

复溶计算器

复溶计算器允许您快速计算试剂的体积，以复溶小瓶。只需输入试剂的质量和目标浓度，计算器将确定其余部分。

体积（添加到小瓶中）

质量（小瓶）

所需的复溶浓度

AZ084

库存信息

库存信息

库存信息

库存信息

基本描述

关联靶点（人）

作用机制

名称和识别符

化学和物理性质

安全和危险性（GHS）

质量标准

质检证书（CoA,COO,BSE/TSE 和分析图谱)

溶液计算器

摩尔浓度计算器

稀释计算器

复溶计算器