IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). IACS-10759 is orally bioavailable with excellent physicochemical properties in preclinical species and achieves significant in vivo efficacy with daily oral dosing of 10-25 mg/kg.
|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|
IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities
Marina P, et al. AACR; Cancer Res. 2015 Aug;Volume 75, Issue 15 Supplement, pp. 4380.
Apilimod mesylate is a potent IL-12/IL-23 inhibitor, which inhibits the IL-12 production in cultures of IFN-γ/LPS–stimulated human PBMCs with an IC50 of 10 nM.
OK432 is a freeze-dried vaccine.
Glycoursodeoxycholic acid, a acyl glycine and a bile acid-glycine conjugate, is a metabolite of ursodeoxycholic acid.
Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a bile acid formed in the liver from chenodeoxycholate and glycine.
Ercalcidiol is a metabolite of vitamin D2, is regarded as an indicator of vitamin D nutritional status.
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