Cat. No.: HY-19775

GNE-6468

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GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC₅₀ value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC₅₀ of 30 nM for IL-17 PBMC.

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Pureté: 98.02%
CAS No.: 1677668-27-7
Formule: C₂₃H₁₆ClN₃O₄
Masse moléculaire:433.84

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GNE-6468 Chemical Structure

CAS No.: 1677668-27-7

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC₅₀ value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC₅₀ of 30 nM for IL-17 PBMC^[1].

IC₅₀ & Target^[1]

ROR-γ

2 nM (EC₅₀)

Voir tous les produits spécifiques à Isoform ROR :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	EC₅₀	>10 μM Compound: 28, GNE-6468	Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 26048793]
HEK-293T	EC₅₀	>10 μM Compound: 28, GNE-6468	Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 26048793]
HEK-293T	EC₅₀	>10 μM Compound: 28, GNE-6468	Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 26048793]
HEK-293T	EC₅₀	>10 μM Compound: 28, GNE-6468	Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 26048793]
HEK-293T	EC₅₀	>10 μM Compound: 28, GNE-6468	Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 26048793]
HEK-293T	EC₅₀	>10 μM Compound: 28, GNE-6468	Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 26048793]
HEK-293T	EC₅₀	0.013 μM Compound: 28, GNE-6468	Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 26048793]
PBMC	EC₅₀	>10 μM Compound: 28, GNE-6468	Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay	[PMID: 26048793]
PBMC	EC₅₀	>10 μM Compound: 28, GNE-6468	Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA	[PMID: 26048793]
PBMC	EC₅₀	0.03 μM Compound: 28, GNE-6468	Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA	[PMID: 26048793]

In Vivo

GNE-6468 (compound 28) displays high predicted clearance values in human and rodent hepatocytes (CL_hep = 17 and 42 mL/min/kg, respectively) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1677668-27-7
Appearance Solid
Masse moléculaire 433.84
Formule C₂₃H₁₆ClN₃O₄
Color Light yellow to yellow
SMILES

OC1=CC(C2=C3N(C(C(C4=C(C5CC5)C=CC=C4Cl)=O)=N2)C=CC=N3)=CC=C1C(O)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Immunity

A chemical agonist and the Golgi-resident lipid PI4P activate STING by inducing transmembrane helix rearrangement. [Abstract]

2025 Dec 5:S1074-7613(25)00506-0. PMID: 41352342

Solvant et solubilité

In Vitro:

DMSO : 5 mg/mL (11.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3050 mL

11.5250 mL

23.0500 mL

5 mM

0.4610 mL

2.3050 mL

4.6100 mL

10 mM

0.2305 mL

1.1525 mL

2.3050 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (251 KB)
- English - EN (251 KB)
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- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Fauber BP, et al. Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists. Bioorg Med Chem Lett. 2015 Aug 1;25(15):2907-12. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3050 mL	11.5250 mL	23.0500 mL	57.6249 mL
	5 mM	0.4610 mL	2.3050 mL	4.6100 mL	11.5250 mL
	10 mM	0.2305 mL	1.1525 mL	2.3050 mL	5.7625 mL

Keywords

GNE-6468

1 Cited Publications

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GNE-6468

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Publications Citing Use of MedChemExpress (MCE) GNE-6468

Voir tous les produits spécifiques à Isoform ROR

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GNE-6468

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Small Molecule Immuno-Oncology Compound Library

Transcription Factor-Targeted Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GNE-6468

Voir tous les produits spécifiques à Isoform ROR

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GNE-6468 Related Classifications

HY-19775 Related Classifications