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.
Triton x-100 is a nonionic, non-denaturing detergent suitable for solubilization, isolation and purification of membrane protein complexes.It is chemically indistinguishable from Nonidet P-40.
Adjudin (also known as AF-2364) is a potent Cl- channel blocker, with a superior mitochondria-inhibitory effect.
2-Phenylethyl isothiocyanate is an NNK-induced lung tumorigenesis inhibitor.
Benzyl isothiocyanate is a naturally-occurring constituent of cruciferous vegetables with antibacterial properties.
Iodixanol is a nonionic hydrophilic compound commonly used as a contrast agent during coronary angiography.
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