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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)
Biological Activity for LY 2955303
LY 2955303 is a 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.
Compound Libraries for LY 2955303
LY 2955303 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LY 2955303
| 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 for LY 2955303
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.57 | 20 |
Preparing Stock Solutions for LY 2955303
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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Product Datasheets for LY 2955303
References for LY 2955303
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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Keywords: LY 2955303, LY 2955303 supplier, LY2955303, selective, retinoic, acid, receptor, gamma, RARg, antagonists, antagonism, osteoarthritis, high, affinity, Retinoic, Acid, Receptors, 5984, Tocris Bioscience
1 Citation for LY 2955303
Citations are publications that use Tocris products. Selected citations for LY 2955303 include:
Takashi et al (2023) Blockage of retinoic acid signaling via RARγ suppressed the proliferation of pancreatic cancer cells by arresting the cell cycle progression of the G1-S phase. Cancer Cell Int 23 94 PMID: 37198667
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Retinoid Receptors Scientific Review
Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.