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trans-ISRIB

Cat. No. M7425
trans-ISRIB Structure
Synonym:

ISRIB (trans)

Size Price Availability Quantity
10mg USD 130  USD130 In stock
25mg USD 230  USD230 In stock
50mg USD 400  USD400 In stock
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Quality Control
Biological Activity

trans-ISRIB is a integrated stress response (ISR) inhibitor; reverses the effects of eIF2α phosphorylation (IC50 = 5 nM) and restores cell translation capacity. Acts downstream of PERK, targeting interactions between eIF2α kinases and elF2B. Blocks ATF4 production without altering the IRE1 or ATF6 responses in vitro. Displays memory enhancement in hippocampus-dependent spatial and fear-associated learning in rodents. Brain penetrant. ISRIB reduces the viability of cells subjected to PERK-activation by chronic endoplasmic reticulum stress. eIF2α phosphorylation is implicated in memory consolidation. Remarkably, ISRIB-treated mice display significant enhancement in spatial and fear-associated learning.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 451.34
Formula C22H24Cl2N2O4
CAS Number 1597403-47-8
Purity >98%
Solubility DMSO 4.5 mg/mL (with gentle warming)
Storage at -20°C
References

[1] Carmela Sidrauski, et al. Elife . Pharmacological brake-release of mRNA translation enhances cognitive memory

[2] Cuzzocrea, et al. Br J Pharmacol. Beneficial effects of 3-aminobenzamide, an inhibitor of poly (ADP-ribose) synthetase in a rat model of splanchnic artery occlusion and reperfusion.

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  Catalog
Abmole Inhibitor Catalog




Keywords: trans-ISRIB, ISRIB (trans) supplier, PERK, inhibitors

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