ISRIB (trans-isomer)|1597403-47-8|-陌孚医药/Medlife

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ISRIB (trans-isomer)

目录号: PL09430 纯度: ≥99%

CAS No. :1597403-47-8

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中文名称	ISRIB (trans-isomer)
中文别名	ISRIB(trans-isomer) 抑制剂;N,N'-(反式-环己烷-1,4-二基)双(2-(4-氯苯氧基)乙酰胺)
英文名称	ISRIB (trans-isomer)
英文别名	trans-ISRIB;ISRIB trans-isomer;ISRIB;ISRIB (trans-isomer);N,N'-(cis-Cyclohexane-1,4-diyl)bis(2-(4-chlorophenoxy)acetamide);N,N'-((1r,4r)-cyclohexane-1,4-diyl)bis(2-(4-chlorophenoxy)acetamide);N,N'-trans-1,4-cyclohexanediylbis[2-(4-chlorophenoxy)acetamide];2-(4-chloranylphenoxy)-~{N}-[4-[2-(4-chloranylphenoxy)ethanoylamino]cyclohexyl]ethanamide;2-(4-chlorophenoxy)-N-(4-{[(4-chlorophenoxy)acetyl]amino}cyclohexyl)acetamide;isrib-trans-isomer;C7B;Oprea1;N,N'-(trans-cyclohexane-1,4-diyl)bis(2-(4-chlorophenoxy)acetamide)
Cas No.	1597403-47-8
分子式	C₂₂H₂₄Cl₂N₂O₄
分子量	451.34
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	ISRIB (trans-isomer)是高效的PERK抑制剂，IC₅₀值为 5 nM。ISRIB 可有效逆转 eIF2α 磷酸化的作用 (IC₅₀=5 nM)。
生物活性	ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC 50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC 50 =5 nM).
性状	Solid
IC50 & Target[1][2]	PERK 5 nM (IC50)
体外研究(In Vitro)	Trans-ISRIB is 100-fold more potent (IC50=5 nM) than cis-ISRIB (IC50= 600 nM), indicating that the compound’s interaction with its cellular target is stereospecific. ISRIB reduces the viability of cells subjected to PERK-activation by chronic endoplasmic reticulum stress. ISRIB substantially reverses the translational effects elicited by phosphorylation of eIF2α and induces no major changes in translation or mRNA levels in unstressed cells. eIF2α phosphorylation-induced stress granule (SG) formation is blocked by ISRIB. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	ISRIB increases long-term memory in rodents. ISRIB-treated mice display significant enhancement in spatial and fear-associated learning. ISRIB displays a half-life in plasma of 8 hr and readily crossed the blood-brain barrier, quickly equilibrating with the central nervous system. 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	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Sidrauski C, et al. Pharmacological brake-release of mRNA translation enhances cognitive memory. Elife. 2013 May 28;2:e00498. [2]. Sidrauski C, et al. The small molecule ISRIB reverses the effects of eIF2α phosphorylation on translation and stressgranule assembly. Elife. 2015 Feb 26;4. doi: 10.7554/eLife.05033.

溶解度数据	In Vitro: DMSO : 4.55 mg/mL (10.08 mM; ultrasonic and warming and heat to 60°C)配制储备液

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