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PSN632408

Cat. No. M3771
PSN632408 Structure
Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 200 In stock
50mg USD 840 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively). PSN632408 has been reported to activate human and mouse GPR119 in a yeast fluorimetric assay with EC50 of 5.6±0.99 μM and 7.9±0.7 μM, respectively. In HEK-OSGPR116 cells, cAMP level was dose-dependently increased by PSN632408 with an EC50 of 1.9±0.14 μM. In vivo, PSN632408 induced food intake reduction by using a rat feeding model and acute hypophagic effects in dose-dependence.PSN632408 may be useful as a therapeutic agent for the treatment of obesity.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 360.41
Formula C18H24N4O4
CAS Number 857652-30-3
Purity >99%
Solubility DMSO
Storage at -20°C
References

Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents.
Overton HA, et al. Cell Metab. 2006 Mar;3(3):167-75. PMID: 16517404.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PSN632408 supplier, GPR, inhibitors

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