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Simufilam dihydrochloride (PTI-125 dihydrochloride) 是口服具有活力的、毒性低的 filamin A 激活剂。它可优先结合改变的 FLNA,并恢复其天然构象,恢复受体和突触活性,并减少其与 a7nAChR/TLR4 的关联和下游病理作用。它可用于研究阿尔茨海默症。
Simufilam dihydrochloride (PTI-125 dihydrochloride) 是口服具有活力的、毒性低的 filamin A 激活剂。它可优先结合改变的 FLNA,并恢复其天然构象,恢复受体和突触活性,并减少其与 a7nAChR/TLR4 的关联和下游病理作用。它可用于研究阿尔茨海默症。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 588 | 现货 | |
5 mg | ¥ 1,470 | 现货 | |
10 mg | ¥ 2,330 | 现货 | |
25 mg | ¥ 3,930 | 现货 | |
50 mg | ¥ 5,720 | 现货 | |
100 mg | ¥ 7,970 | 现货 | |
200 mg | ¥ 10,700 | 现货 | |
500 mg | ¥ 15,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,490 | 现货 |
产品描述 | Simufilam dihydrochloride (PTI-125 dihydrochloride) is a low toxicity, orally active filamin A (FLNA) activator, which can be used for the research of Alzheimer's disease. Simufilam dihydrochloride preferentially binds altered FLNA and restores its native conformation, restoring receptor and synaptic activities and reducing its α7nAChR/TLR4 associations and downstream pathologies. |
体外活性 | Simufilam dihydrochloride (1 pM~1 nM)以剂量依赖的方式增加NMDA/甘氨酸诱导的Arc表达。Simufilam dihydrochloride (1 nM, 1小时)大大恢复了filamin A到其原生构象,并有效地正常化了AD前额皮层中的受体活性。Simufilam dihydrochloride 以剂量依赖的方式降低了Ab42诱导的FLNA与a7nAChR及TLR4的耦合,在Ab42处理的对照组和AD海马体中均有此现象。Simufilam dihydrochloride 降低了Ab42对a7nAChR的结合亲和力,从而阻止了Ab42的信号传导和在a7nAChRs上的进一步积累。 |
体内活性 | Simufilam dihydrochloride(22 mg/kg;口服)显著减少FLNAea7nAChR/TLR4的关联。Simufilam dihydrochloride显著改善空间记忆力。 |
别名 | PTI-125 dihydrochloride |
分子量 | 332.3 |
分子式 | C15H23Cl2N3O |
CAS No. | 2480226-06-8 |
Smiles | [H]Cl.O=C1N(CC2=CC=CC=C2)C3(CCN(C)CC3)NC1.[H]Cl |
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: 65 mg/ml (195.61 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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