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Exicorilant Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5754853

Exicorilant is a selective and oral active glucocorticoid receptor (GR) antagonist (Ki: 7nM) and it also has the potential to overcome adiposity, glucose intolerance, and dyslipidemia. More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Exicorilant, Inhibitor
Full Product Name
Exicorilant
Product Synonym Names
CORT 125281
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
589.56
Solubility
DMSO: 250mg/mL (424.05mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C26H23F4N7O3S
SMILES
O=C([C@]12CC3=C(N(C4=CC=C(F)C=C4)N=C3)C[C@]1([H])CCN(S(=O)(C5=NN(C)N=C5)=O)C2)C6=NC=CC(C(F)(F)F)=C6
CAS Number
1781244-77-6
Target & IC50
GR: ic50 7nM (ki)
In Vitro
Exicorilant decreases fat mass, body weight, and plasma lipids in HFD-fed mice. Exicorilant (6, 20, or 60mg/kg/d, for 3 weeks in mice) at different dosages reduce fat mass, body weight, plasma TG, cholesterol, and FFA in a dose-dependent manner. But it has no effect on lean mass [2].

Product References and Citations for Exicorilant, inhibitor

Hunt HJ, et al. Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. J Med Chem. 2017 Apr 27;60(8):3405-3421.
Hunt HJ, et al. Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. J Med Chem. 2017 Apr 27;60(8):3405-3421.
Kroon J, et al. Selective Glucocorticoid Receptor Antagonist CORT125281 Activates Brown Adipose Tissue and Alters Lipid Distribution in Male Mice. Endocrinology. 2018 Jan 1;159(1):535-546.
Kroon J, et al. Selective Glucocorticoid Receptor Antagonist CORT125281 Activates Brown Adipose Tissue and Alters Lipid Distribution in Male Mice. Endocrinology. 2018 Jan 1;159(1):535-546.

Other Notes

Small volumes of Exicorilant, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

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MBS5754853 is an inhibitor targeting Exicorilant.
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