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Purity: ≥98%
GNE-0946 (GNE0946) is a novel, potent and selective RORγ( RORc) inverse agonist with the potential to be used for treating autoimmune diseases. It activates RORγ with an EC50 value of 4 nM in HEK-293 cells. The nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORγ, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in the production of the pro-inflammatory cytokine interleukin-17. GNE-0946 displayed >300-fold selectivity for RORc over the other ROR family members, PPARγ, and NRs in our cellular selectivity panel. The favorable potency, selectivity, and physiochemical properties of GNE-0946 and GNE-6468, in addition to their potent suppression of IL-17 production in human primary cells, support their use as chemical biology tools to further explore the role of RORc in human biology.
| References |
Bioorg Med Chem Lett.2015 Aug 1;25(15):2907-12.
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| Molecular Formula |
C22H12CLF3N2O4
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| Molecular Weight |
460.789895057678
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| CAS # |
1677667-24-1
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| SMILES |
ClC1=CC=CC(C(F)(F)F)=C1C(C1=NC(C2C=CC(C(=O)O)=C(C=2)O)=C2C=CC=CN21)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~217.02 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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