CORT-108297

  • CAT Number: I006191
  • CAS Number: 1018679-79-2
  • Molecular Formula: C26H25F4N3O3S
  • Molecular Weight: 535.56
  • Purity: ≥95%
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CORT-108297 (Cat.No:I006191), also known as ADS-108297 and C-108927, is a cortisol receptor (GR-II) antagonist potentially for the mitigation of antipsychotic induced obesity.

Catalog Number I006191
CAS Number 1018679-79-2
Molecular Formula

C26H25F4N3O3S

Purity 95%
Target cortisol receptor antagonist
Solubility Soluble in DMSO
Storage 0 - 4°C for short term ,or -20 °C for long term
IUPAC Name (4aR)-4a-(ethoxymethyl)-1-(4-fluorophenyl)-6-[4-(trifluoromethyl)phenyl]sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinoline
InChI InChI=1S/C26H25F4N3O3S/c1-2-36-17-25-14-18-15-31-33(22-7-5-21(27)6-8-22)24(18)13-20(25)11-12-32(16-25)37(34,35)23-9-3-19(4-10-23)26(28,29)30/h3-10,13,15H,2,11-12,14,16-17H2,1H3/t25-/m1/s1
InChIKey SLKURXRZHJOZOD-RUZDIDTESA-N
SMILES CCOCC12CC3=C(C=C1CCN(C2)S(=O)(=O)C4=CC=C(C=C4)C(F)(F)F)N(N=C3)C5=CC=C(C=C5)F
Reference

1:Horm Behav. 2014 Apr;65(4):363-71. doi: 10.1016/j.yhbeh.2014.02.002. Epub 2014 Feb 11. The selective glucocorticoid receptor antagonist CORT 108297 decreases neuroendocrine stress responses and immobility in the forced swim test.Solomon MB,Wulsin AC,Rice T,Wick D,Myers B,McKlveen J,Flak JN,Ulrich-Lai Y,Herman JP, PMID: 24530653 PMCID: PMC4074011 DOI: 10.1016/j.yhbeh.2014.02.002 </br><span>Abstract:</span> Pre-clinical and clinical studies have employed treatment with glucocorticoid receptor (GR) antagonists in an attempt to limit the deleterious behavioral and physiological effects of excess glucocorticoids. Here, we examined the effects of GR antagonists on neuroendocrine and behavioral stress responses, using two compounds: mifepristone, a GR antagonist that is also a progesterone receptor antagonist, and CORT 108297, a specific GR antagonist lacking anti-progestin activity. Given its well-documented impact on neuroendocrine and behavioral stress responses, imipramine (tricyclic antidepressant) served as a positive control. Male rats were treated for five days with mifepristone (10mg/kg), CORT 108297 (30mg/kg and 60mg/kg), imipramine (10mg/kg) or vehicle and exposed to forced swim test (FST) or restraint stress. Relative to vehicle, imipramine potently suppressed adrenocorticotropin hormone (ACTH) responses to FST and restraint exposure. Imipramine also decreased immobility in the FST, consistent with antidepressant actions. Both doses of CORT 108297 potently suppressed peak corticosterone responses to FST and restraint stress. However, only the higher dose of CORT 108297 (60mg/kg) significantly decreased immobility in the FST. In contrast, mifepristone induced protracted secretion of corticosterone in response to both stressors, and modestly decreased immobility in the FST. Taken together, the data indicate distinct effects of each compound on neuroendocrine stress responses and also highlight dissociation between corticosterone responses and immobility in the FST. Within the context of the present study, our data suggest that CORT 108297 may be an attractive alternative for mitigating neuroendocrine and behavioral states associated with excess glucocorticoid secretion. Copyright © 2014 Elsevier Inc. All rights reserved.

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