| Hazard Information | Back Directory | [Uses]
CRN04894 (compound 17h) is an orally active MC2R antagonist that demonstrates in vivo efficacy in rat model of adrenocorticotropic hormone (ACTH)-stimulated corticosterone secretion[1]. CRN04894 binds to human or rat MC2R with KB values of 0.34 nM and 0.23 nM, respsectively[1]. | [in vivo]
CRN04894 (compound 17h) (3, 30 mg/kg; po; single dose) dose-dependently reduces corticosterone secretion levels in an ACTH-stimulated male rat model[1].
| Animal Model: | Adrenocorticotrophic hormone (ACTH)-stimulated corticosterone secretion in Male Sprague-Dawley Rats[1] | | Dosage: | 3 mg/kg, 30 mg/kg | | Administration: | po; single dose; ACTH(1-24) stimulated at 4 hr after CRN04894 treatment. | | Result: | Significantly decreased the concentration level of corticosterone via oral administration.br/
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| [IC 50]
rat MC2R: 0.23 nM (Kb); MC2R: 0.34 nM (Kb) | [References]
[1] Kim SH, et al. Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist. ACS Med Chem Lett. 2024 Mar 19;15(4):478-485. DOI:10.1021/acsmedchemlett.3c00514 |
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