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BioChemicals
Cort108297
tcsc0008503
Cort108297
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AVAILABLE SIZES
1mg
5mg
10mg
$
2,951.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
Cort108297 is a specific
glucocorticoid receptor
(
GR
) antagonist. Cort108297 has a high affinity for GRs with a
K
i
of 0.45 nM.
IC50 & Target: Ki: 0.45 nM (glucocorticoid receptor)
[1]
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)
[2]
.
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
[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. 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)
[4]
.
Information
CAS No
1018679-79-2
Formula
C
26
H
25
F
4
N
3
O
3
S
Clinical Information
clinicalinformation
Pathway
GPCR/G Protein
Target
Glucocorticoid Receptor
Specifications
Purity / Grade
>98%
Solubility
10 mM in DMSO
Smiles
smiles
Misc Information
Observed Molecular Weight
535.55
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