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GSK2033

Cat. No. M6768
GSK2033 Structure
Synonym:

GSK 2033

Size Price Availability Quantity
5mg USD 115  USD115 In stock
10mg USD 190  USD190 In stock
25mg USD 310  USD310 In stock
50mg USD 500  USD500 In stock
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Quality Control & Documentation
Biological Activity

GSK2033 is a potent LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively. GSK2033 enhances T-cell proliferation and blocks T 0901317-antiproliferative activity on T-cells. GSK2033 is cell permeable.

Product Citations
Chemical Information
Molecular Weight 591.66
Formula C29H28F3NO5S
CAS Number 1221277-90-2
Solubility (25°C) DMSO 22 mg/mL (Need warming)
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] Kristine Griffett, et al. Biochem Biophys Res Commun. Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver disease

[2] Consoli, et al. Eur.J Pharmacol. Behavioral effects of the β3 adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs?.

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Keywords: GSK2033, GSK 2033 supplier, Liver X Receptor, inhibitors, activators


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