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GSK575594A

Cat. No. M8271
GSK575594A Structure
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Biological Activity

GSK575594A is a selective agonist of human GPR55. It is specific for human over rodent GPR55. GSK575594A had no activity across a set of more than 200 validated molecular target assays from diverse classes including kinases, proteases and other enzymes, GPCRs, ion channels, nuclear receptors, and membrane transporters.

Chemical Information
Molecular Weight 471.52
Formula C24H23F2N3O3S
CAS Number 909418-68-4
Solubility (25°C) DMSO: ≥5 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] Strahinja Stevanovic, et al. Potential modulating effect of the Ascaris suum nicotinic acetylcholine receptor (nAChR) by compounds GSK575594A, diazepam and flumazenil discovered by structure-based virtual screening approach

[2] Andrew J Brown, et al. Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist

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