LY2955303 - CAS 1433497-19-8
Catalog number: 1433497-19-8
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C36H42N4O3
Molecular Weight:
578.76
COA:
Inquire
Targets:
RAR/RXR
Description:
LY2955303 is a selective Retinoic acid receptor gamma (RAR-γ) antagonist with Ki of 1.09 nM; (RAR-α Ki > 1700 nM; RAR-β Ki > 2980 nM). LY2955303 showed good pharmacokinetic properties and was efficacious in the MIA model of osteoarthritis-like joint pain. It can be used for the treatment of osteoarthritis pain.
Purity:
98%
Appearance:
Powder
Synonyms:
LY2955303; LY-2955303; LY 2955303. 4-(5-(3,5-di-tert-butylphenyl)-1-(4-(4-methylpiperazine-1-carbonyl)phenyl)-1H-pyrazol-3-yl)benzoic acid
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
osteoarthritis pain
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Canonical SMILES:
O=C(O)C1=CC=C(C2=NN(C3=CC=C(C(N4CCN(C)CC4)=O)C=C3)C(C5=CC(C(C)(C)C)=CC(C(C)(C)C)=C5)=C2)C=C1
1.Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design.
Hughes NE;Bleisch TJ;Jones SA;Richardson TI;Doti RA;Wang Y;Stout SL;Durst GL;Chambers MG;Oskins JL;Lin C;Adams LA;Page TJ;Barr RJ;Zink RW;Osborne H;Montrose-Rafizadeh C;Norman BH Bioorg Med Chem Lett. 2016 Jul 15;26(14):3274-3277. doi: 10.1016/j.bmcl.2016.05.056. Epub 2016 May 20.
A series of triaryl pyrazoles were identified as potent pan antagonists for the retinoic acid receptors (RARs) α, β and γ. X-ray crystallography and structure-based drug design were used to improve selectivity for RARγ by targeting residue differences in the ligand binding pockets of these receptors. This resulted in the discovery of novel antagonists which maintained RARγ potency but were greater than 500-fold selective versus RARα and RARβ. The potent and selective RARγ antagonist LY2955303 demonstrated good pharmacokinetic properties and was efficacious in the MIA model of osteoarthritis-like joint pain. This compound demonstrated an improved margin to RARα-mediated adverse effects.
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