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INCB13739

Cat. No. M21098
INCB13739  Structure
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Biological Activity

INCB13739 is an orally effective, selective and tissue-specific 11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor with IC50 values of 3.2 nM (11β-HSD1 enzyme) and 1.1 nM (11β-HSD1 PBMC), respectively.INCB13739 can be used in type 2 diabetes mellitus (T2DM) and obesity studies.

Chemical Information
Molecular Weight 467.52
Formula C28H25N3O4
CAS Number 869974-19-6
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] Colin Zhang, et al. Bioorg Med Chem Lett. Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach

[2] G Hollis, et al. Diabetes Obes Metab. 11β-Hydroxysteroid dehydrogenase type 1 inhibition in type 2 diabetes mellitus

[3] Julio Rosenstock, et al. Diabetes Care. The 11-beta-hydroxysteroid dehydrogenase type 1 inhibitor INCB13739 improves hyperglycemia in patients with type 2 diabetes inadequately controlled by metformin monotherapy

[4] Atul Tiwari. IDrugs. INCB-13739, an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of type 2 diabetes

[5] R Ge, et al. Curr Med Chem. 11beta-hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development

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Keywords: INCB13739 supplier, Hydroxysteroid dehydrogenase, inhibitors, activators


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