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GW3965 

Cat. No. M30052
GW3965  Structure
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Biological Activity

GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.

Chemical Information
Molecular Weight 582.05
Formula C33H31ClF3NO3
CAS Number 405911-09-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Zhikun Zhan, et al. Pharmacol Res. Oridonin alleviates hyperbilirubinemia through activating LXRα-UGT1A1 axis

[2] Sevtap Han, et al. Life Sci. The effects of LXR agonist GW3965 on vascular reactivity and inflammation in hypertensive rat aorta

[3] Yong Hu, et al. Oncotarget. Liver X receptors agonist GW3965 re-sensitizes gefitinib-resistant human non-small cell lung cancer cell to gefitinib treatment by inhibiting NF-κB in vitro

[4] Xu Cui, et al. Stroke. ABCA1/ApoE/HDL Pathway Mediates GW3965-Induced Neurorestoration After Stroke

[5] Xu Cui, et al. Stroke. The neurorestorative benefit of GW3965 treatment of stroke in mice

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Keywords: GW3965  supplier, Liver X Receptor, inhibitors, activators


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