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GSK1034702

Cat. No. M42668
GSK1034702 Structure
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Biological Activity

GSK1034702 is a M1 mAChR allosteric agonist.

Chemical Information
Molecular Weight 333.4
Formula C18H24FN3O2
CAS Number 932373-87-0
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] Sophie J Bradley et al. Mol Pharmacol. Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes

[2] Michael J Hobbs et al. Xenobiotica. Retrospective use of PBPK modelling to understand a clinical drug-drug interaction between dextromethorphan and GSK1034702

[3] Khanum Ridler et al. EJNMMI Res. An evaluation of the brain distribution of [(11)C]GSK1034702, a muscarinic-1 (M 1) positive allosteric modulator in the living human brain using positron emission tomography

[4] Pradeep J Nathan et al. Int J Neuropsychopharmacol. The potent M1 receptor allosteric agonist GSK1034702 improves episodic memory in humans in the nicotine abstinence model of cognitive dysfunction

[5] Mickael Huiban et al. Appl Radiat Isot. Fully automated synthesis of the M₁ receptor agonist [¹¹C]GSK1034702 for clinical use on an Eckert & Ziegler Modular Lab system

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Keywords: GSK1034702 supplier, AChR/AChE, inhibitors, activators


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