LY 2955303

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Cat.No. 5984 - LY 2955303 | C36H42N4O3 | CAS No. 1433497-19-8
Description: High affinity and selective RARγ antagonist
Chemical Name: 4-[5-[3,5-Bis(1,1-dimethylethyl)phenyl]-1-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-1H-pyrazol-3-yl]benzoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

High affinity and selective RARγ antagonist (Ki values are 1.1 nM, >1.7 μM and >2.9 μM for RARγ, RARα and RARβ respectively). Displays analgesic efficacy in a mouse model of osteoarthritis-like joint pain.

Technical Data

M. Wt 578.74
Formula C36H42N4O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1433497-19-8
PubChem ID 71552369
InChI Key YVXYHNKIOFSFMZ-UHFFFAOYSA-N
Smiles CN1CCN(C(C2=CC=C(N3N=C(C4=CC=C(C(O)=O)C=C4)C=C3C5=CC(C(C)(C)C)=CC(C(C)(C)C)=C5)C=C2)=O)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.57 20

Preparing Stock Solutions

The following data is based on the product molecular weight 578.74. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 8.64 mL 43.2 mL 86.39 mL
1 mM 1.73 mL 8.64 mL 17.28 mL
2 mM 0.86 mL 4.32 mL 8.64 mL
10 mM 0.17 mL 0.86 mL 1.73 mL

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References

References are publications that support the biological activity of the product.

Hughes et al (2016) Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design. Bioorg.Med.Chem.Letts. 26 3274 PMID: 27261179


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