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Submit ReviewLY 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.
LY 2955303 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 578.74 |
公式 | C36H42N4O3 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 11.57 | 20 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for LY 2955303, please let us know.
关键词: LY 2955303, LY 2955303 supplier, LY2955303, selective, retinoic, acid, receptor, gamma, RARg, antagonists, antagonism, osteoarthritis, high, affinity, Retinoic, Acid, Receptors, 5984, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 LY 2955303 的部分引用包括:
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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