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ABT-384 

Cat. No. M30757
ABT-384  Structure
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Biological Activity

ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD).

Chemical Information
Molecular Weight 493.56
Formula C25H34F3N5O2
CAS Number 868623-40-9
Form Solid
Solubility (25°C) DMSO 31.25 mg/mL (ultrasonic and warming and heat to 60°C)
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] Guohua An, et al. J Clin Pharmacol. Small-molecule compounds exhibiting target-mediated drug disposition - A case example of ABT-384

[2] Guohua An, et al. Biopharm Drug Dispos. Population pharmacokinetics of the 11β-hydroxysteroid dehydrogenase type 1 inhibitor ABT-384 in healthy volunteers following single and multiple dose regimens

[3] Gerard J Marek, et al. Alzheimers Dement. Efficacy and safety evaluation of HSD-1 inhibitor ABT-384 in Alzheimer's disease

[4] D A Katz, et al. Transl Psychiatry. Peripheral and central nervous system inhibition of 11β-hydroxysteroid dehydrogenase type 1 in man by the novel inhibitor ABT-384

[5] Guohua An, et al. Drug Metab Dispos. Effect of ketoconazole on the pharmacokinetics of the 11β-hydroxysteroid dehydrogenase type 1 inhibitor ABT-384 and its two active metabolites in healthy volunteers: population analysis of data from a drug-drug interaction study

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Keywords: ABT-384  supplier, Hydroxysteroid dehydrogenase, inhibitors, activators

 
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