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CX546

Cat. No. M7707
CX546 Structure
Synonym:

CX-546; GR-87

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50mg USD 420  USD420 4-7 Days
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Quality Control & Documentation
Biological Activity

CX546 is a selective positive AMPA glutamate receptor modulator. CX546 caused an approximately 2-fold increase in the affinity for radiolabeled agonists, whereas CX516 was ineffective. CX546 enhances cognitive function in rats. Administration of CX546 improved the disrupted LI in mGluR5 knockout mice and facilitated LI in control C57BL/6J mice, given extended number of conditioning trails.

Chemical Information
Molecular Weight 247.29
Formula C14H17NO3
CAS Number 215923-54-9
Solubility (25°C) Ethanol ≥ 10 mg/mL
DMSO ≥ 10 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] Tatiana Lipina, et al. Neuropsychopharmacology. The ampakine CX546 restores the prepulse inhibition and latent inhibition deficits in mGluR5-deficient mice

[2] Amy C Arai, et al. J Pharmacol Exp Ther. Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action

[3] J C Lauterborn, et al. J Neurosci. Positive modulation of AMPA receptors increases neurotrophin expression by hippocampal and cortical neurons

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Keywords: CX546, CX-546; GR-87 supplier, GluR, inhibitors, activators


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