PT2385 inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31).
|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: ≥ 40 mg/mL|
Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis.
Xie C, et al. Nat Med. 2017 Nov;23(11):1298-1308. PMID: 29035368.
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