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Rimiducid 是一种可渗透脂质的他克莫司类似物,是一种二聚剂,通过交联 FKBP 结构域起作用。它将 Caspase 9 自杀开关二聚化并迅速诱导细胞凋亡。
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Rimiducid 是一种可渗透脂质的他克莫司类似物,是一种二聚剂,通过交联 FKBP 结构域起作用。它将 Caspase 9 自杀开关二聚化并迅速诱导细胞凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 568 | 现货 | |
2 mg | ¥ 837 | 现货 | |
5 mg | ¥ 1,690 | 现货 | |
10 mg | ¥ 2,860 | 现货 | |
25 mg | ¥ 4,750 | 现货 | |
50 mg | ¥ 6,780 | 现货 | |
100 mg | ¥ 9,190 | 现货 |
产品描述 | Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis. |
靶点活性 | FKBP:(EC50)0.1 nM |
体外活性 | AP1903, a bivalent 'dimerizer' drug that binds FKBP and induces Fas cross-linking.?A single 2-hour treatment eliminated approximately 80% of T cells, and multiple exposures induced further apoptosis.?T cells were eliminated regardless of their proliferation state, suggesting that the AP1903/Fas system, which contains only human components, is a promising alternative to HSV-tk for treating GVHD[2]. |
体内活性 | 持续的hGH分泌为监测活体内可存活细胞数量提供了一种便捷准确的方法,因为在小鼠中hGH的血清半衰期仅约3分钟。我们连续3天将这些细胞通过肌内(i.m.)植入裸鼠,并通过静脉(i.v.)给予不同剂量的Rimiducid处理这些动物,然后测定血清hGH水平以评估存活细胞的数量。Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, 和 100 mg/kg)引发的血清人类GH水平降低呈剂量依赖性,半最大有效剂量为0.4±0.1 mg/kg[1]。 |
分子量 | 1411.63 |
分子式 | C78H98N4O20 |
CAS No. | 195514-63-7 |
Smiles | CC[C@H](C(=O)N1CCCC[C@H]1C(=O)O[C@H](CCc1ccc(OC)c(OC)c1)c1cccc(OCC(=O)NCCNC(=O)COc2cccc(c2)[C@@H](CCc2ccc(OC)c(OC)c2)OC(=O)[C@@H]2CCCCN2C(=O)[C@@H](CC)c2cc(OC)c(OC)c(OC)c2)c1)c1cc(OC)c(OC)c(OC)c1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (35.42 mM), Sonication is recommended. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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