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SAFit1 

Cat. No. M28764
SAFit1  Structure
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Biological Activity

SAFit1 is a FK506 binding protein 51 (FKBP51)-specific inhibitor with a Ki of 4±0.3 nM.

Chemical Information
Molecular Weight 747.87
Formula C42H53NO11
CAS Number 1643125-32-9
Form Solid
Solubility (25°C) DMSO ≥ 300 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] Bhavesh Babulal Gabani, et al. Drug Res (Stuttg). Validated LC-MS/MS Method for Simultaneous Quantitation of SAFit-1 and SAFit-2 in Mice Plasma: Application to a Pharmacokinetic Study

[2] Cherno O Sidibeh, et al. Endocrine. FKBP5 expression in human adipose tissue: potential role in glucose and lipid metabolism, adipogenesis and type 2 diabetes

[3] Steffen Gaali, et al. Nat Chem Biol. Selective inhibitors of the FK506-binding protein 51 by induced fit

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  Catalog
Abmole Inhibitor Catalog




Keywords: SAFit1  supplier, FKBP (FK506-binding protein), inhibitors, activators


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