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Cort108297

🥰Excellent
Catalog No. T15000Cas 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).

Cort108297

Cort108297

🥰Excellent
Purity: 98%
Catalog No. T15000Cas 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).
Pack SizePriceAvailabilityQuantity
1 mg$289In Stock
5 mg$655In Stock
10 mg$955In Stock
25 mg$1,490In Stock
50 mg$1,980In Stock
100 mg$2,890In Stock
1 mL x 10 mM (in DMSO)$787In Stock
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Purity:98%
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Product Introduction

Bioactivity
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
GR:(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].
Chemical Properties
Molecular Weight535.55
FormulaC26H25F4N3O3S
Cas No.1018679-79-2
SmilesCCOC[C@@]12CN(CCC1=Cc1c(C2)cnn1-c1ccc(F)cc1)S(=O)(=O)c1ccc(cc1)C(F)(F)F
Relative Density.1.40 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 30 mg/mL (56.02 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8672 mL9.3362 mL18.6724 mL93.3620 mL
5 mM0.3734 mL1.8672 mL3.7345 mL18.6724 mL
10 mM0.1867 mL0.9336 mL1.8672 mL9.3362 mL
20 mM0.0934 mL0.4668 mL0.9336 mL4.6681 mL
50 mM0.0373 mL0.1867 mL0.3734 mL1.8672 mL

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