Free shipping on all orders over $ 500

SKI2852 

Cat. No. M28211
SKI2852  Structure
Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50s of 1.6 nM and 2.9 nM against mHSD1 and hHSD1, respectively.

Chemical Information
Molecular Weight 543.65
Formula C27H34FN5O4S
CAS Number 1346554-47-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Je Ho Ryu, et al. J Med Chem. Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydroge䲧瘀Ỵ瘁㧀痿羹皘

[2] Seon-Mi Kim, et al. J Med Chem. Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist

[3] Hyunhee Oh, et al. Eur J Pharmacol. A potent and selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, SKI2852, ameliorates metabolic syndrome in diabetic mice models

Related Hydroxysteroid dehydrogenase Products
ARO-HSD

ARO-HSD is an siRNA and also an inhibitor of 17β-HSD13 that can be used in studies related to non-alcoholic steatohepatitis (NASH).

ALN-HSD

ALN-HSD is an siRNA and also an inhibitor of 17β-hydroxysteroid dehydrogenase 13 (17β-HSD13), which can be used in studies related to non-alcoholic steatohepatitis (NASH).

ABT-384 

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).

SCH-451659 

SCH-451659 is an inhibitor of 17β-hydroxysteroid dehydrogenases (17β-HSDs) for cancer research.

BI‑3231 

BI 3231 is a potent and selective hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor, with IC50s of 1 and 13 nM for hHSD17B13 and mHSD17B13, respectively. BI 3231 has the potential for the research of nonalcoholic steatohepatitis (NASH) and other liver diseases.

  Catalog
Abmole Inhibitor Catalog




Keywords: SKI2852  supplier, Hydroxysteroid dehydrogenase, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.