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16α-Hydroxyprednisolone

Cat. No. M28325
16α-Hydroxyprednisolone Structure
Synonym:

OH-PRED

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Biological Activity

16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes.

Chemical Information
Molecular Weight 376.44
Formula C21H28O6
CAS Number 13951-70-7
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, protect from light
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] Odile Francesca Restaino, et al. Molecules. Biotechnological Transformation of Hydrocortisone into 16α-Hydroxyprednisolone by Coupling Arthrobacter simplex and Streptomyces roseochromogenes

[2] No authors listed. Triamcinolone

[3] No authors listed. Triamcinolone, Topical

[4] Teresa Gazzotti, et al. MethodsX. An LC-MS/MS method for the determination of budesonide and 16α-hydroxyprednisolone in dog plasma

[5] K Deventer, et al. J Pharm Biomed Anal. Detection of budesonide in human urine after inhalation by liquid chromatography-mass spectrometry

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Keywords: 16α-Hydroxyprednisolone, OH-PRED supplier, Metabolite/Endogenous Metabolite, inhibitors, activators


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