3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
- CAS号:941575-71-9
- 英文名:3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
- 中文名:3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
- CBNumber:CB42695130
- 分子式:C21H13BrN2O3
- 分子量:421.24
- MOL File:941575-71-9.mol
- 沸点 :643.5±55.0 °C(Predicted)
- 密度 :1?+-.0.1 g/cm3(Predicted)
- 储存条件 :room temp
- 溶解度 :DMSO: ≥15mg/mL
- 形态 :powder
- 酸度系数(pKa) :7.44±0.60(Predicted)
- 颜色 :light orange to dark orange
3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione性质、用途与生产工艺
- 生物活性 BIP-135 是一个高效、选择性的,ATP 竞争性的 GSK-3 抑制剂,对 GSK-3α 和 GSK-3β 作用的IC50 值分别为 16 nM 和 21 nM。BIP 135 具有神经保护作用。
-
靶点
GSK-3α
16 nM (IC 50 )
GSK-3β
21 nM (IC 50 )
-
体外研究
BIP-135 (20-30 μM; 72 hours) increases the survival motor neuron (SMN) protein levels at a dose of 25 μM in human SMA fibroblasts. And the typical bell-shaped dose-response curve is observed due to some toxicity at higher concentrations.
BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress.
Western Blot Analysis
Cell Line: Human SMA fibroblasts Concentration: 20 μM, 25 μM, 30 μM Incubation Time: 72 hours Result: Led to a 7-fold increase in SMN levels at 25 μM. -
体内研究
BIP-135 does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight).
BIP-135 (75 mg/kg; i.p.; daily; from postnatal day 0 to 21) prolongs the median survival time of Δ7 SMA KO mouse model of spinal muscular atrophy.
Animal Model: Male and female SMN2 +/+ , SMN2Δ7 +/+ , Smn +/– mice Dosage: 75 mg/kg Administration: Intraperitoneal injection; daily; from postnatal day 0 to 21 Result: Caused a modest extension in the median survival of SMA KO animals by two days.
- 更新日期:2024/04/30
- 产品编号:HY-111055
- 产品名称:3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione BIP-135
- CAS编号:941575-71-9
- 包装:1mg
- 价格:681元
- 更新日期:2024/04/30
- 产品编号:HY-111055
- 产品名称:3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione BIP-135
- CAS编号:941575-71-9
- 包装:10mg
- 价格:2400元
- 公司名称:TORONTO
- 联系电话:--
- 电子邮件:info@trc-canada.com
- 国家:加拿大
- 产品数:6088
- 优势度:71