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Relacorilant

Chemical Structure : Relacorilant

CAS No.: 1496510-51-0

Relacorilant (CORT125134, CORT 125134)

Catalog No.: PC-22512Not For Human Use, Lab Use Only.

Relacorilant (CORT125134) is a potent, selective and orally bioavailable glucocorticoid receptor modulator (SGRM) with Ki of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Relacorilant (CORT125134) is a potent, selective and orally bioavailable glucocorticoid receptor modulator (SGRM) with Ki of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay.
Relacorilant (CORT125134) has no progesterone receptor activity.
Relacorilant (CORT125134) reverses the glucocorticoid-mediated anti-apoptotic effects and restores the taxane chemosensitivity in epithelial ovarian cancer cells.
Relacorilant (CORT125134) improved the efficacy of paclitaxel and the potency of platinum agents in OVCAR5 cell line.
Relacorilant (CORT125134) increased tumor-cell apoptosis when combined with paclitaxel in multiple models including MIA PaCa-2, HeLa, and a cholangiocarcinoma patient-derived xenograft.

Physicochemical Properties

M.Wt 586.57
Formula C27H22F4N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-1,4,5,6,7,8-hexahydro-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone

References

1. Pivonello R, et al. Front Endocrinol (Lausanne). 2021 Jul 14;12:662865.

2. Greenstein AE, et al. Oncotarget. 2021 Jun 22;12(13):1243-1255.

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