A PPARβ/δ antagonist
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GSK0660

Item No. 15272

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[[2-methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid, methyl ester
CAS Number
1014691-61-2
Molecular Formula
C19H18N2O5S2
Formula Weight
418.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 12 mg/mlEthanol: 2 mg/ml
λmax
286 nm
SMILES
O=S(NC(C=C1)=C(OC)C=C1NC2=CC=CC=C2)(C3=C(C(OC)=O)SC=C3)=O
InChi Code
InChI=1S/C19H18N2O5S2/c1-25-16-12-14(20-13-6-4-3-5-7-13)8-9-15(16)21-28(23,24)17-10-11-27-18(17)19(22)26-2/h3-12,20-21H,1-2H3
InChi Key
NDFKBGWLUHKMFY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $107

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    10 mg

    $201

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    25 mg

    $470

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    50 mg

    $783

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    Product Description

    GSK0660 is the first reported antagonist of PPARβ/δ (IC50 = 155 nM) with no measurable affinity for PPARα or PPARγ (IC50s ≥ 10 μM).1 Because of the limited bioavailability of GSK0660, the related compound GSK3787 (Item No. 15219) was developed as a selective PPARβ/δ antagonist with more suitable pharmacokinetic properties.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shearer, B.G., Steger, D.J., Way, J.M., et al. Identification and characterization of a selective peroxisome proliferator-activated receptor b/d (NR1C2) antagonist. Mol. Endocrinol. 22(2), 523-529 (2008).

    2. Palkar, P.S., Borland, M.G., Naruhn, S., et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-β/δ antagonist GSK3787. Mol. Pharmacol. 78(3), 419-430 (2010).