2BAct|2143542-28-1|-陌孚医药/Medlife

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2BAct

目录号: PL14816 纯度: ≥98%

CAS No. :2143542-28-1

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中文名称	2BAct
英文名称	2BAct
英文别名	2BAct;N-(3-(2-(4-Chloro-3-fluorophenoxy)acetamido)bicyclo[1.1.1]pentan-1-yl)-5-(difluoromethyl)pyrazine-2-carboxamide;N-[3-[[2-(4-chloro-3-fluorophenoxy)acetyl]amino]-1-bicyclo[1.1.1]pentanyl]-5-(difluoromethyl)pyrazine-2-carboxamide
Cas No.	2143542-28-1
分子式	C₁₉H₁₆ClF₃N₄O₃
分子量	440.80
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情	2BAct 是一种具有高选择性的，具有口服活性的真核起始因子 eIF2B 活化剂，EC₅₀ 为 33 nM。2BAct 可防止由慢性综合应激反应引起的神经系统缺陷。2BAct 可透过血脑屏障。2BAct 相对于 eIF2B 激活剂 ISRIB (HY-12495) 显示出更好的溶解度和药代动力学性质。
生物活性	2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC 50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct is able to penetrate the central nervous system (CNS). 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB (HY-12495).
性状	Solid
IC50 & Target[1][2]	EC50: 33 nM (eIF2B)
体外研究(In Vitro)	Primary fibroblast lysates from R191H embryos has lower GEF activity than WT lysates, and 2BAct enhances this activity threefold (EC50=7.3 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	2BAct (300 μg 2BAct/g of meal; 21 weeks) normalizes body weight gain in VWM mice. 2BAct prevents the appearance of motor deficits, myelin loss and reactive gliosis in VWM mice. 2BAct stimulates the remaining activity of mutant eIF2B complex in vivo, abrogating the maladaptive stress response. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献	[1]. Wong YL, et al. eIF2B activator prevents neurological defects caused by a chronic integrated stress response. Elife. 2019;8:e42940. Published 2019 Jan 9.

溶解度数据	In Vitro: DMSO : 250 mg/mL (567.15 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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