ISRIB(trans-isomer)

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ISRIB(trans-isomer)

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1597403-47-8

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

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 ofPERKwith anIC₅₀of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC₅₀=5 nM).

IC₅₀& Target^[1]

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^[1]. 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^[2].

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^[1].

分子量

451.34

性状

Solid

Formula

C₂₂H₂₄Cl₂N₂O₄

CAS 号

1597403-47-8

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
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 4.55 mg/mL(10.08 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。