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Fig. 1 · Structure
Cat. No.
A20780
CAS No.
1677668-27-7
Formula
C23H16ClN3O4
Mol. Weight
433.84

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GNE-6468

Cat. No. A20780 CAS 1677668-27-7

RORγ(RORc) agonists

GNE-6468 is a potent and selective RORγ(RORc) agonists with an EC50 value of 13 nM for HEK-293 cell.

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Biological Activity

Target & Activity

Target Activity Value
ROR-γ EC50 2 nM

Cellular Effect

Cell Line Activity Value Description Reference
HEK-293T EC50 > 10 μM 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 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 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 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 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 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 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 Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay [PMID: 26048793]
PBMC EC50 > 10 μM Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA [PMID: 26048793]
PBMC EC50 0.03 μM Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA [PMID: 26048793]

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Specifications

Manufacturer Adooq Bioscience
Actions Agonist
CAS Number 1677668-27-7
Applications RORγ(RORc) agonists
Formula C23H16ClN3O4
Molecular Weight 433.84
SMILES
OC1=CC(C2=C3N(C(C(C4=C(C5CC5)C=CC=C4Cl)=O)=N2)C=CC=N3)=CC=C1C(O)=O

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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