A potent RARγ antagonist
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LY2955303

Item No. 25833

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[5-[3,5-bis(1,1-dimethylethyl)phenyl]-1-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-1H-pyrazol-3-yl]-benzoic acid
CAS Number
1433497-19-8
Molecular Formula
C36H42N4O3
Formula Weight
578.7
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 25 mg/ml
λmax
285 nm
SMILES
CN1CCN(C(C2=CC=C(N3C(C4=CC(C(C)(C)C)=CC(C(C)(C)C)=C4)=CC(C5=CC=C(C(O)=O)C=C5)=N3)C=C2)=O)CC1
InChi Code
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)
InChi Key
YVXYHNKIOFSFMZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $103

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    10 mg

    $186

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    25 mg

    $420

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    Product Description

    LY2955303 is a potent antagonist of retinoic acid receptor γ (RARγ; Ki = 1.1 nM).1 It is selective for RARγ over RARα and RARβ (Kis = >1,700 and >2,980 nM, respectively). LY2955303 reduces differential weight bearing between the contralateral and ipsilateral limbs in a rat model of monoiodoacetate-induced osteoarthritis (ED50 = 0.72 mg/kg).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hughes, N.E., Bleisch, T.J., Jones, S.A., 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. 26(14), 3274-3277 (2016).