| 产品描述: | Rimiducid (AP1903) 是一种化学蛋白二聚体,可与 FKBP 融合蛋白 紧密结合,同时与丰富的天然 FKBP 结合最少。Rimiducid 在表达二聚体依赖的 Fas 构建体的培养物中引发有效且剂量依赖的细胞凋亡,EC50 约为 0.1 nM |
| 靶点: |
FKBP fusion protein |
| 体外研究: |
Rimiducid (AP1903) induces effective and dose-dependent apoptosis in the culture expressing dimer-dependent Fas constructors, indicating that Rimiducid causes the activation of Fas signaling without interference from endogenous FKBP. |
| 体内研究: |
Rimiducid (AP1903) elicits a dose-dependent decrease in serum hGH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg, which means AP1903 is functional of activating of Fas signaling in vivo |
| 细胞实验: |
Cell lines: HT1080 cells Concentrations: 0.01-1000 nM Incubation Time: Overnight Method: HT1080 cells stably transduced with retrovirus pSR a-myr-2FKBP-Fas-E (open circles) or pSR a-myr-2 (F36V-FKBP)- Fas-E (closed circles) were treated overnight with AP1903, and viability then was measured by Alamar Blue assay. |
| 动物实验: |
Animal Models: Nude mice implanted with hGH-secreting HTFasGH-3 cells Dosages: 2 ml/kg Administration: i.v. |
| 参考文献: |
1. J D Iuliucci, et al. Intravenous safety and pharmacokinetics of a novel dimerizer drug, AP1903, in healthy volunteers. J Clin Pharmacol. 2001 Aug;41(8):870-9. 2. T Clackson, et al. Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10437-42. |
| 溶解性: |
Soluble in DMSO、Ethanol |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
0.708 ml |
3.542 ml |
7.084 ml |
| 5 mM |
0.142 ml |
0.708 ml |
1.417 ml |
| 10 mM |
0.071 ml |
0.354 ml |
0.708 ml |
| 50 mM |
0.014 ml |
0.071 ml |
0.142 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |