Cat. No.: HY-19774

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GNE-0946

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GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC₅₀ value of 4 nM for HEK-293 cell.

For research use only. We do not sell to patients.

Purity: 98.11%
CAS No.: 1677667-24-1
Formula: C₂₂H₁₂ClF₃N₂O₄
Molecular Weight:460.79

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GNE-0946 Chemical Structure

CAS No.: 1677667-24-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC₅₀ value of 4 nM for HEK-293 cell.

All ROR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	EC₅₀	>10 μM Compound: 9, GNE-0946	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: 9, GNE-0946	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: 9, GNE-0946	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: 9, GNE-0946	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: 9, GNE-0946	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: 9, GNE-0946	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	0.004 μM Compound: 9, GNE-0946	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: 9, GNE-0946	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: 9, GNE-0946	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	0.017 μM Compound: 9, GNE-0946	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]

Chemical Information

CAS No. 1677667-24-1
Appearance Solid
Molecular Weight 460.79
Formula C₂₂H₁₂ClF₃N₂O₄
Color Light yellow to green yellow
SMILES

OC1=CC(C2=C3N(C(C(C4=C(C(F)(F)F)C=CC=C4Cl)=O)=N2)C=CC=C3)=CC=C1C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (217.02 mM; ultrasonic and warming and heat to 60°C; 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

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1702 mL

10.8509 mL

21.7019 mL

5 mM

0.4340 mL

2.1702 mL

4.3404 mL

10 mM

0.2170 mL

1.0851 mL

2.1702 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- 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)
Handling Instructions (2659 KB)

References

[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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1702 mL	10.8509 mL	21.7019 mL	54.2546 mL
	5 mM	0.4340 mL	2.1702 mL	4.3404 mL	10.8509 mL
	10 mM	0.2170 mL	1.0851 mL	2.1702 mL	5.4255 mL
	15 mM	0.1447 mL	0.7234 mL	1.4468 mL	3.6170 mL
	20 mM	0.1085 mL	0.5425 mL	1.0851 mL	2.7127 mL
	25 mM	0.0868 mL	0.4340 mL	0.8681 mL	2.1702 mL
	30 mM	0.0723 mL	0.3617 mL	0.7234 mL	1.8085 mL
	40 mM	0.0543 mL	0.2713 mL	0.5425 mL	1.3564 mL
	50 mM	0.0434 mL	0.2170 mL	0.4340 mL	1.0851 mL
	60 mM	0.0362 mL	0.1808 mL	0.3617 mL	0.9042 mL
	80 mM	0.0271 mL	0.1356 mL	0.2713 mL	0.6782 mL
	100 mM	0.0217 mL	0.1085 mL	0.2170 mL	0.5425 mL

Keywords

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GNE-0946

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

All ROR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GNE-0946

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

All ROR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GNE-0946 Related Classifications

HY-19774 Related Classifications