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LY2812223 

Cat. No. M28154
LY2812223  Structure
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Biological Activity

LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).

Chemical Information
Molecular Weight 284.29
Formula C10H12N4O4S
CAS Number 1311385-20-2
Form Solid
Solubility (25°C) Water 50 mg/mL (ultrasonic)
DMSO 28.75 mg/mL (ultrasonic)
Storage -20°C, sealed
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] Juliet McColm, et al. Br J Clin Pharmacol. Evaluation of single and multiple doses of a novel mGlu2 agonist, a potential antipsychotic therapy, in healthy subjects

[2] Christian C Felder, et al. J Pharmacol Exp Ther. Translational Pharmacology of the Metabotropic Glutamate 2 Receptor-Preferring Agonist LY2812223 in the Animal and Human Brain

[3] James A Monn, et al. J Med Chem. Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812䲧瘀Ỵ瘁㧀痿羹皘的ࡍţࡍĀ�皚嶁皖Ѐ瑖犤

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Keywords: LY2812223  supplier, GluR, inhibitors, activators


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