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Glucocorticoid receptor agonist

Cat. No. M13980
Glucocorticoid receptor agonist Structure
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Biological Activity

Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist. IC50 value: Target:

Chemical Information
Molecular Weight 396.38
CAS Number 1245526-82-2
Solubility (25°C) DMSO ≥ 90 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] Chaoyun Pan, et al. Cisplatin-mediated activation of glucocorticoid receptor induces platinum resistance via MAST1

[2] Kevin N Dack, et al. Topical 'dual-soft' glucocorticoid receptor agonist for dermatology

[3] Onno C Meijer, et al. Glucocorticoid receptor modulators

[4] Peter J Barnes. Glucocorticosteroids

[5] Robert H Oakley, et al. The biology of the glucocorticoid receptor: new signaling mechanisms in health and disease

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