LY 2955303

Names

[ CAS No. ]:
1433497-19-8

[ Name ]:
LY 2955303

Biological Activity

[Description]:

LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> RAR/RXR

Research Areas >> Others

[Target]

Ki: 1.09 nM (RARγ)[1]

[In Vitro]

LY2955303 is tested and observed that the binding Kis for RARα, RARβ and RARγ are >1700, >2980 and 1.09 nM, respectively. The functional Ki for RARγ is 7.1±4.9 nM[1].

[In Vivo]

A single oral dose of LY2955303 demonstrates a dose responsive effect whereby the rat reduces differential weight bearing (ED50=0.72 mg/kg)[1].

[References]

[1]. Hughes NE, et al. 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 Lett. 2016 Jul 15;26(14):3274-3277.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₆H₄₂N₄O₃

[ Molecular Weight ]:
578.74

[ Storage condition ]:
2-8℃

Safety Information

[ Hazard Codes ]:
Xn

LY 2955303

Names

Biological Activity

Chemical & Physical Properties

Safety Information

Related Compounds