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LY2119620 

Cat. No. M30813
LY2119620  Structure
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Biological Activity

LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.

Chemical Information
Molecular Weight 437.94
Formula C19H24ClN5O3S
CAS Number 886047-22-9
Form Solid
Solubility (25°C) DMSO 67.5 mg/mL (ultrasonic)
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] Jun Xu, et al. Nat Commun. Structural and dynamic insights into supra-physiological activation and allosteric modulation of a muscarinic acetylcholine receptor

[2] Jingjing Wang, et al. Nat Commun. The unconventional activation of the muscarinic acetylcholine receptor M4R by diverse ligands

[3] Quan Li, et al. RSC Adv. Synergistic regulation mechanism of iperoxo and LY2119620 for muscarinic acetylcholine M2 receptor

[4] Douglas A Schober, et al. Mol Pharmacol. Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites

[5] Carrie H Croy, et al. Mol Pharmacol. Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors

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