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GSK0660

Cat. No. M2732
GSK0660 Structure
Size Price Availability Quantity
5mg USD 70  USD70 In stock
10mg USD 110  USD110 In stock
50mg USD 420  USD420 In stock
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Quality Control & Documentation
Biological Activity

GSK0660 is a selective PPARδ antagonist with IC50 of 155 nM.

Chemical Information
Molecular Weight 418.49
Formula C19H18N2O5S2
CAS Number 1014691-61-2
Solubility (25°C) DMSO 90 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Chuang Yang, et al. PPARβ down-regulation is involved in high glucose-induced endothelial injury via acceleration of nitrative stress

[2] Danyang Tian, et al. Endogenous hydrogen sulfide improves vascular remodeling through PPARδ/SOCS3 signaling

[3] Megan E Capozzi, et al. The peroxisome proliferator-activated receptor-β/δ antagonist GSK0660 mitigates retinal cell inflammation and leukostasis

[4] Sara R Savage, et al. RNA-seq identifies a role for the PPARβ/δ inverse agonist GSK0660 in the regulation of TNFα-induced cytokine signaling in retinal endothelial cells

[5] Xiao-Chen Bao, et al. Protective role of peroxisome proliferator-activated receptor-β/δ against pulmonary oxygen toxicity mediated through changes in NOS expression levels

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  Catalog
Abmole Inhibitor Catalog




Keywords: GSK0660 supplier, PPAR, inhibitors, activators


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