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Trofinetide是一种衍生自具有神经保护作用的三肽Gly-Pro-Glu的化合物,后者是胰岛素样生长因子-1(IGF-1)的N-端序列。在10 nM的浓度下使用时,它能减少由蛋白磷酸酶抑制剂奥卡达酸在原代大鼠胚胎纹状体神经元中引起的细胞死亡。Trofinetide在一种由穿透性弹道样脑损伤引起的大鼠神经炎症模型中减少了编码IL-1β、TNF-α、IL-6和E-selectin的mRNA的脑表达。在通过中脑动脉闭塞(MCAO)引起的大鼠脑损伤模型中,以30和60 mg/kg的剂量给药时,它减少了皮层和纹状体梗塞区域。Trofinetide(每天100 mg/kg)减少了树突棘的数量,并逆转了在fmr1-/-敲除小鼠脆性X综合征模型中的社交识别和情景恐惧条件反射的缺陷,同时也减少了睾丸重量的增加。含有Trofinetide的制剂已被用于治疗Rett综合征。
Trofinetide是一种衍生自具有神经保护作用的三肽Gly-Pro-Glu的化合物,后者是胰岛素样生长因子-1(IGF-1)的N-端序列。在10 nM的浓度下使用时,它能减少由蛋白磷酸酶抑制剂奥卡达酸在原代大鼠胚胎纹状体神经元中引起的细胞死亡。Trofinetide在一种由穿透性弹道样脑损伤引起的大鼠神经炎症模型中减少了编码IL-1β、TNF-α、IL-6和E-selectin的mRNA的脑表达。在通过中脑动脉闭塞(MCAO)引起的大鼠脑损伤模型中,以30和60 mg/kg的剂量给药时,它减少了皮层和纹状体梗塞区域。Trofinetide(每天100 mg/kg)减少了树突棘的数量,并逆转了在fmr1-/-敲除小鼠脆性X综合征模型中的社交识别和情景恐惧条件反射的缺陷,同时也减少了睾丸重量的增加。含有Trofinetide的制剂已被用于治疗Rett综合征。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 2,400 | 期货 | |
5 mg | ¥ 10,700 | 期货 | |
10 mg | ¥ 19,000 | 期货 | |
25 mg | ¥ 41,700 | 期货 |
产品描述 | Trofinetide, derived from the neuroprotective tripeptide Gly-Pro-Glu (an N-terminal sequence of insulin-like growth factor-1, IGF-1), shows promise in various neuroprotective models. At a concentration of 10 nM, it mitigates cell death in primary rat embryonic striatal neurons caused by okadaic acid. Additionally, Trofinetide reduces the expression of pro-inflammatory markers (IL-1β, TNF-α, IL-6, and E-selectin) in a rat model simulating neuroinflammation from penetrating ballistic-like brain injuries. In cases of brain injury induced by middle cerebral artery occlusion (MCAO), administration of Trofinetide at 30 and 60 mg/kg reduces the area of cortical and striatal infarct. Furthermore, a daily dose of 100 mg/kg reverses social recognition and contextual fear conditioning deficits, diminishes the number of dendritic spines, and decreases testicular weight gain in an fmr1-/- knockout mouse model of fragile X syndrome. Trofinetide formulations have been employed in treating Rett syndrome, highlighting its versatility across various neurological conditions. |
别名 | NNZ-2566 |
分子量 | 315.32 |
分子式 | C13H21N3O6.XC2H4O2 |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | Ethanol: 1 mg/ml PBS pH 7.2: 10 mg/ml DMSO: 10 mg/ml DMF: 5 mg/ml |
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