ISRIB
目录号 : GC10581
ISRIB是PERK信号抑制剂
Cas No.:548470-11-7
Sample solution is provided at 25 µL, 10mM.
IC50: 5 nM
ISRIB is a potent inhibitor of PERK signaling.
As one of the four eIF2α kinases in mammalian cells, PERK responds to an accumulation of unfolded proteins in the endoplasmic reticulum.
In vitro: Compared with cis-ISRIB, trans-ISRIB proved 100-fold more potent (IC50 = 5 nM vs IC50 = 600 nM), suggesting that ISRIB interacted with its cellular target stereospecifically. In addition, ISRIB could block the production of endogenous ATF4, while had no obvious effect on XBP1 mRNA splicing and XBP1s production. Meanwhile, ISRIB did not affect activation of the ATF6-branch of the UPR, however, ISRIB could block the downstream of PERK and eIF2α phosphorylation [1].
In vivo: In mouse with a single intraperitoneal injection, ISRIB showed a plasma half-life of 8 hr and readily crossed the blood-brain barrier with quick equilibrium in the central nervous system. The detected brain ISRIB concentrations were found to be several fold higher than its IC50. Moreover, ISRIB-treated mice displayed significant enhancement in spatial and fear-associated learning. Therefore, memory consolidation was inherently limited by the ISR, and ISRIB could release suchbrake. These results showed that ISRIB might contribute to the understanding and treatment of cognitive disorders [1].
Clinical trial: Up to now, ISRIB is still in the preclinical development stage.
Reference:
[1] Sidrauski C, et al. Pharmacological brake-release of mRNA translation enhances cognitive memory. Elife. 2013 May 28;2:e00498.
| Cas No. | 548470-11-7 | SDF | |
| 化学名 | (1Z,1'Z)-N',N''-((1r,4r)-cyclohexane-1,4-diyl)bis(2-(4-chlorophenoxy)acetimidic acid) | ||
| Canonical SMILES | ClC1=CC=C(OC/C(O)=N/[C@@]2([H])CC[C@@](/N=C(O)/COC3=CC=C(Cl)C=C3)([H])CC2)C=C1 | ||
| 分子式 | C22H24Cl2N2O4 | 分子量 | 451.34 |
| 溶解度 | ≥ 15.03mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2156 mL | 11.0781 mL | 22.1562 mL |
| 5 mM | 0.4431 mL | 2.2156 mL | 4.4312 mL |
| 10 mM | 0.2216 mL | 1.1078 mL | 2.2156 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet