ISO-1 significantly blocked photoreceptor apoptosis, outer nuclear layer (ONL) thinning, and retinal gliosis. ISO-1 and MIF knockout (MIFKO) had greater accumulation of Müller glia pERK expression in the detached retina. ISO-1 significantly inhibits the cytokine activity in vitro. In vivo, administration of ISO-1 resulted in a significant reduction in implant size and vascularity (as assessed by Flk1 mRNA expression) which was not associated with an alteration in the reproductive cycle in mice.
|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: ≥ 30 mg/mL|
Inhibition of macrophage migration inhibitory factor reduces endometriotic implant size in mice with experimentally induced disease.
Nothnick WB, et al. J Endometr. 2011 Sep 30;3(3):135-142. PMID: 24790725.
ISO-1 binding to the tautomerase active site of MIF inhibits its pro-inflammatory activity and increases survival in severe sepsis.
Al-Abed Y, et al. J Biol Chem. 2005 Nov 4;280(44):36541-4. PMID: 16115897.
S107 is a Type 1 ryanodine receptor (RyR1) stabilizer.
3,3’,5,5’-Tetramethylbenzidine(TMB) is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualising reagent used in enzyme-linked immunosorbent assays (ELISA).
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.
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