GNE-6468

Name: GNE-6468
Brand: MedChemExpress
SKU: HY-19775
Rating: 4.5 (1 reviews)

Cat. No.: HY-19775 Purity: 98.04%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

GNE-6468 Chemical Structure

CAS No. : 1677668-27-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 418	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 418	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 620	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1700	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2550	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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RORγ RORα RORβ

Biological Activity
Purity & Documentation
References
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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)

Cellular Effect

Cell Line	Type	Value	Description	References
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	> 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	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 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 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 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	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.

Molecular Weight

433.84

Formula

C₂₃H₁₆ClN₃O₄

CAS No.

1677668-27-7

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.04%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (258 KB) LCMS (89 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]

Complete Stock Solution Preparation Table

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

GNE-6468 Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-64681677668-27-7GNE6468GNE 6468RORRAR-related orphan receptorRORcPPARγIL-17PBMCInhibitorinhibitorinhibit

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GNE-6468

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Biological Activity

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References

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Complete Stock Solution Preparation Table

GNE-6468 Related Classifications

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