TM6008 is a prolyl hydroxylase (PHD) inhibitor that protects against cell death after hypoxia. TM6008 suppresses the activity of PHDs, inducing continuous HIF-1α activation. Immunoblotting revealed that TM6008 increased the expression of HIF-1α, HIF-2α and vascular endothelial growth factor in myocarditis.
In vivo, TM6008 improved left ventricular ejection fraction significantly on the 21st day of EAM. Though TM6008 did not affect the severity of myocardial cell infiltration, it tended to reduce cardiac fibrosis. Immunohistochemistry showed that CD31-positive blood vessels were preserved in the TM6008 group compared to the control group. Immunoblotting revealed that TM6008 increased the expression of HIF-1α, HIF-2α and vascular endothelial growth factor in myocarditis. Oral administration of TM6008 protected neurons in a model of cerebrovascular disease.
|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.
Neovascularization induced by hypoxia inducible transcription factor is associated with the improvement of cardiac dysfunction in experimental autoimmune myocarditis.
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A novel prolyl hydroxylase inhibitor protects against cell death after hypoxia.
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Takizawa S, et al. Rinsho Shinkeigaku. 2012;52(11):911-2. PMID: 23196464.
Inhibition of prolyl hydroxylase domain-containing protein suppressed lipopolysaccharide-induced TNF-alpha expression.
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A novel class of prolyl hydroxylase inhibitors induces angiogenesis and exerts organ protection against ischemia.
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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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