LY2955303

LY2955303
Identifiers
	IUPAC name 4-[5-(3,5-di-tert-butylphenyl)-1-[4-(4-methylpiperazine-1-carbonyl)phenyl]-1H-pyrazol-3-yl]benzoic acid;
CAS Number	1433497-19-8;
PubChem CID	71552369;
UNII	EGR6ZG7M0Z;
ChEMBL	ChEMBL3814815;
Chemical and physical data
Formula	C36H42N4O3
Molar mass	578.757 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)(C)C1=CC(=CC(=C1)C2=CC(=NN2C3=CC=C(C=C3)C(=O)N4CCN(CC4)C)C5=CC=C(C=C5)C(=O)O)C(C)(C)C;
	InChI InChI=1S/C36H42N4O3/c1-35(2,3)28-20-27(21-29(22-28)36(4,5)6)32-23-31(24-8-10-26(11-9-24)34(42)43)37-40(32)30-14-12-25(13-15-30)33(41)39-18-16-38(7)17-19-39/h8-15,20-23H,16-19H2,1-7H3,(H,42,43); Key:YVXYHNKIOFSFMZ-UHFFFAOYSA-N;

LY2955303 is a drug which acts as a potent and selective antagonist of the retinoic acid receptor γ (RARγ). It inhibits the signalling pathway of the pro-inflammatory mediator NF-κB and has been researched as a potential treatment for arthritis.^[1]^[2]

References

↑ Hughes NE, Bleisch TJ, Jones SA, Richardson TI, Doti RA, Wang Y, et al. (15 July 2016). "Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design". Bioorganic & Medicinal Chemistry Letters. 26 (14): 3274–3277. doi:10.1016/j.bmcl.2016.05.056. OSTI 1430391. PMID 27261179.
↑ Yu YW, Li SY, Zhang LJ, Wang QL, Liu ZG, Chen QZ, et al. (7 November 2022). "Retinoic Acid Receptor Gamma (RARγ) Promotes Cartilage Destruction through Positive Feedback Activation of NF-κB Pathway in Human Osteoarthritis". Mediators of Inflammation. 2022 1875736. doi:10.1155/2022/1875736. PMC 9663240. PMID 36387933.

[1] Hughes NE, Bleisch TJ, Jones SA, Richardson TI, Doti RA, Wang Y, et al. (15 July 2016). "Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design". Bioorganic & Medicinal Chemistry Letters. 26 (14): 3274–3277. doi:10.1016/j.bmcl.2016.05.056. OSTI 1430391. PMID 27261179.

[2] Yu YW, Li SY, Zhang LJ, Wang QL, Liu ZG, Chen QZ, et al. (7 November 2022). "Retinoic Acid Receptor Gamma (RARγ) Promotes Cartilage Destruction through Positive Feedback Activation of NF-κB Pathway in Human Osteoarthritis". Mediators of Inflammation. 2022 1875736. doi:10.1155/2022/1875736. PMC 9663240. PMID 36387933.

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