Cort108297

CAS No. 1018679-79-2

Cort108297( —— )

Catalog No. M33322 CAS No. 1018679-79-2

Cort108297 is a selective glucocorticoid receptor modulator and a selective GR antagonist with no affinity for other steroid receptors. Cort108297 showed a high affinity for GRs (Ki: 0.45nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 439 Get Quote
5MG 622 Get Quote
10MG 907 Get Quote
25MG 1371 Get Quote
50MG 1822 Get Quote
100MG 2601 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Cort108297
  • Note
    Research use only, not for human use.
  • Brief Description
    Cort108297 is a selective glucocorticoid receptor modulator and a selective GR antagonist with no affinity for other steroid receptors. Cort108297 showed a high affinity for GRs (Ki: 0.45nM).
  • Description
    Cort108297 is a specific glucocorticoid receptor (GR) antagonist. Cort108297 has a high affinity for GRs with a Ki of 0.45 nM.
  • In Vitro
    In LAPC4 cells, co-treatment with Dexamethasone induces steady-state SGK1 expression 1.7-fold compared to R1881/Enzalutamide (RE) treatment alone. Addition of CORT118335 (1μM) inhibits Dexamethasone-induced SGK1 expression 50% while Cort108297 completely blocks the Dexamethasone-mediated SGK1 increase (p<0.05). KLK3 expression is increased 2.5-fold by Dexamethasone compared to treatment with RE. Both Cort108297 and CORT118335 antagonize Dexamethasone-induced KLK3 expression (by 48% and 60%, respectively, p<0.05). Following 3 days of Dexamethasone±SGRMs in CWR-22Rv1 cells, SGK1 gene expression is dramatically induced by ~100-fold compared to RE-treated cells and this induction is completely abrogated by both Cort108297 and CORT118335 (p<0.01). KLK3 is also induced (7.5-fold) by Dexamethasone compared to RE in CWR-22Rv1 cells; Cort108297 and CORT118335 inhibits this induction by 70% and 75%, respectively (p<0.01).
  • In Vivo
    Ten-week-old, male, C57BL/6J mice are fed a diet containing 60% fat calories and water supplemented with 11% sucrose for 4 weeks. Groups (n=8) receive one of the following: Cort108297 (80?mg/kg QD), Cort108297 (40?mg/kg BID), Mifepristone (30?mg/kg BID), Rosiglitazone (10?mg/kg QD), or vehicle. Compared to mice receiving a high-fat, high-sugar diet plus vehicle, mice receiving a high-fat, high-sugar diet plus either Mifepristone or Cort108297 gain significantly less weight. At the end of the four week treatment period, mice receiving Cort108297 40?mg/kg BID or Cort108297 80?mg/kg QD also have significantly lower steady plasma glucose than mice receiving vehicle. Male rats are treated for five days with Mifepristone (10 mg/kg), Cort108297 (30 mg/kg and 60 mg/kg), Imipramine (10mg/kg) or vehicle and exposed to forced swim test (FST) or restraint stress. Both doses of Cort108297 potently suppress peak corticosterone responses to FST and restraint stress. However, only the higher dose of Cort108297 (60mg/kg) significantly decreases immobility in the forced swim test (FST) .
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Glucocorticoid Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1018679-79-2
  • Formula Weight
    535.55
  • Molecular Formula
    C26H25F4N3O3S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CCOC[C@@]12CN(CCC1=Cc1c(C2)cnn1-c1ccc(F)cc1)S(=O)(=O)c1ccc(cc1)C(F)(F)F
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Sindelar DK, et al. LLY-2707, a novel nonsteroidal glucocorticoid antagonist that reduces atypical antipsychotic-associated weight gain in rats. J Pharmacol Exp Ther. 2014 Jan;348(1):192-201.?
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