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Cort108297

Catalog No. T15000   CAS 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).

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Cort108297 Chemical Structure
Cort108297, CAS 1018679-79-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 289.00
5 mg In stock $ 655.00
10 mg In stock $ 955.00
25 mg In stock $ 1,490.00
50 mg In stock $ 1,980.00
100 mg In stock $ 2,890.00
1 mL * 10 mM (in DMSO) In stock $ 787.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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).
Targets&IC50 Glucocorticoid receptor:(ki)0.45 nM
In vitro Cort108297 and CORT118335 had antagonistic effects on dexamethasone-induced KLK3 expression, which were 48% (p<0.05) and 60% (p<0.05), respectively. CORT118335(1µM) inhibited dexamethasone-induced SGK1 expression by 50%. However, Cort108297 was able to completely inhibit dexamethasone-mediated SGK1 elevation (p<0.05). After 3 days of dexamethasone ±SGRMs treatment in CWR-22RV1 cells, the induction effect of SGK1 gene expression was 100 times greater than that in re treated cells, while Cort108297 and CORT118335 completely inhibited this effect (p<0.01). Cort108297 and CORT118335 inhibited 70% and 75% of induction effects, respectively (p<0.01)[1].
In vivo At the end of the treatment period, mice treated with Cort108297(40 mg/kg BID) or Cort108297 (80 mg/kg QD) also have significantly lower steady plasma glucose than mice receiving vehicle[3]. 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. Experimental data showed that both doses of Cort108297 can effectively inhibit corticosterone response to FST and restraint stress, while only high dose of Cort108297 (60mg/kg) can significantly reduce immobility in forced swimming test (FST). [1].
Molecular Weight 535.55
Formula C26H25F4N3O3S
CAS No. 1018679-79-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (56.02 mM)

TargetMolReferences and Literature

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. 2. Kach J, et al. Selective Glucocorticoid Receptor Modulators (SGRMs) Delay Castrate-Resistant Prostate Cancer Growth. Mol Cancer Ther. 2017 Aug;16(8):1680-1692. 3. Asagami T, et al. Selective Glucocorticoid Receptor (GR-II) Antagonist Reduces Body Weight Gain in Mice. J Nutr Metab. 2011;2011:235389. 4. Solomon MB, et al. The selective glucocorticoid receptor antagonist CORT 108297 decreases neuroendocrine stress responses and immobility in the forced swim test. Horm Behav. 2014 Apr;65(4):363-71.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Bioactive Compound Library Anti-Cancer Compound Library Clinical Compound Library Nuclear Receptor Compound Library Bioactive Compounds Library Max

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Keywords

Cort108297 1018679-79-2 Endocrinology/Hormones Glucocorticoid Receptor Cort-108297 inhibitor inhibit

 

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