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Tarenflurbil

Cat. No. M14524
Tarenflurbil Structure
Synonym:

(R)-Flurbiprofen; MPC7869

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Quality Control & Documentation
Biological Activity

Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.

Chemical Information
Molecular Weight 244.26
CAS Number 51543-40-9
Solubility (25°C) DMSO ≥ 50 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] Mukta Agrawal, et al. Nose-to-brain drug delivery: An update on clinical challenges and progress towards approval of anti-Alzheimer drugs

[2] Mary Sano. Tarenflurbil: mechanisms and myths

[3] Bruno Vellas. Tarenflurbil for Alzheimer's disease: a "shot on goal" that missed

[4] Xu Zhao, et al. Tarenflurbil protection from cytotoxicity is associated with an upregulation of neurotrophins

[5] Paul S Aisen. Tarenflurbil: a shot on goal

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Keywords: Tarenflurbil, (R)-Flurbiprofen; MPC7869 supplier, RAR/RXR, inhibitors, activators


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