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GSK1521498

Cat. No. M21653
GSK1521498 Structure
Synonym:

GSK1521498 free base

Size Price Availability Quantity
5mg USD 340  USD340 In stock
10mg USD 640  USD640 In stock
50mg USD 1950  USD1950 In stock
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Quality Control & Documentation
Biological Activity

GSK1521498 is a potent and selective μ-opioid receptor antagonist. GSK1521498 dose-dependently reduced both cue-controlled alcohol seeking and alcohol intake in the instrumental context as well as alcohol intake in the choice procedure.

Chemical Information
Molecular Weight 402.44
Formula C24H20F2N4
CAS Number 1007573-18-3
Solubility (25°C) DMSO ≥ 6 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Tamzin L Ripley, et al. Psychopharmacology (Berl). The novel mu-opioid antagonist, GSK1521498, reduces ethanol consumption in C57BL/6J mice

[2] Eamonn Kelly, et al. Psychopharmacology (Berl). The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours

[3] Hisham Ziauddeen, et al. J Clin Pharmacol. The effects of alcohol on the pharmacokinetics and pharmacodynamics of the selective mu-opioid receptor antagonist GSK1521498 in healthy subjects

[4] Pradeep J Nathan, et al. J Clin Pharmacol. Multiple-dose safety, pharmacokinetics, and pharmacodynamics of the μ-opioid receptor inverse agonist GSK1521498

[5] Diane M Ignar, et al. J Pharmacol Exp Ther. Regulation of ingestive behaviors in the rat by GSK1521498, a novel micro-opioid receptor-selective inverse agonist

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  Catalog
Abmole Inhibitor Catalog




Keywords: GSK1521498, GSK1521498 free base supplier, Opioid Receptor, inhibitors, activators


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