AP1903

(1R,1'R)-((((Ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
195514-63-7

询价 1g 起订

江苏更新日期：2022-10-22

江苏艾康生物医药研发有限公司

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产品详情:

中文名称：: AP1903

英文名称：: (1R,1'R)-((((Ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)

CAS号：: 195514-63-7

纯度规格：: 95+%

CAS	195514-63-7
中文名称	AP1903
英文名称	(1R,1'R)-((((Ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
储存条件	2-8°C
沸点	1307.5±65.0 °C(Predicted)
酸度系数(pKa)	13.70±0.46(Predicted)
靶点	EC50: 0.1 nM (FKBP, in HT1080 cells) Fas receptor
生物活性	Rimiducid (AP1903) 是二聚化剂，其通过交联 FKBP 结构域起作用，启动 Fas 信号传导，引起凋亡。Rimiducid (AP1903) 使 Caspase 9 自杀开关二聚化，并迅速诱导细胞凋亡 (apoptosis)。
体内研究	Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum human GH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg.
体外研究	The human fibrosarcoma line HT1080 is engineered to express stably a fusion protein comprising a myristoylation sequence, two copies of F36V-FKBP, and the human first apoptosis signal (Fas) intracellular domain. Rimiducid (AP1903) elicits potent and dose-dependent apoptotic death of these engineered cells in culture, with an EC ₅₀ of ≈0.1 nM. Maximal killing occurred in the presence of 3 to 10 nM Rimiducid (AP1903), and the IC ₅₀ is approximately 0.2 nM. LV′VFas-transduced T lymphocytes expressing high levels of CD25 (top panel) are eliminated by with 66%±7.5% (n=10) efficiency. When cells are examined after CD25 expression returned to basal levels, 63%±4.7% (n=9) killing is observed after Rimiducid treatment.

AP1903;AP1903价格;AP1903厂家;195514-63-7

公司简介

医药中间体

成立日期	(12年)
注册资本	1000万人民币
员工人数	1-10人
年营业额	￥ 100万以内
经营模式	贸易,试剂,定制
主营行业	中间体,分子砌块