GSK2981278 is a strong RORγ-selective inverse agonist that inhibits activation of the il17 promoter. GSK2981278 robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level. GSK2981278 attenuates inflammation in a mouse model of psoriasis. Topical treatment with GSK2981278 will significantly limit Th17-type cytokine expression.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 10 mM|
Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin.
Smith SH, et al. PLoS One. 2016 Feb 12;11(2):e0147979. PMID: 26870941.
Coelenterazine is the luciferin, the light-emitting molecule, used for monitoring reporter genes in BRET, ELISA and HTS techniques.
Fluorescein is a synthetic organic compound and dye.
SBI-0640756 is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.
UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator, which inhibits the invasive capacity of carcinoma cells with a Ki of 0.41 μM.
CID5721353 is a B-Cell Lymphoma 6 inhibitor with IC50 of 212 μM.
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