Azaserine is an inhibitor of the rate limiting step of the hexosamine biosynthethic pathway (HBP) and an irreversible inhibitor of GGT1 (gamma-Glutamyltranspeptidase). Azaserine is a naturally occurring serine derivative diazo compound with antineoplastic properties, Azaserine functions as a purine antagonist and glutamine analogue (glutamine amidotransferase inhibitor) that competitively inhibits pathways in which glutamine is metabolized. Azaserine has been shown to elevate the SOD-2 (manganese-superoxide dismutase (MnSOD)) protein level as well as inhibit the oxidative stress and the expression of VCAM-1 and ICAM-1 in response to TNFα. Research indicates that azaserine has the potential to be used as a probe for identifying the L-(leucine-favoring) system transporter in human T-lymphocytes.
|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||Water ≥ 30 mg/mL|
The hexosamine biosynthesis inhibitor azaserine prevents endothelial inflammation and dysfunction under hyperglycemic condition through antioxidant effects.
Rajapakse AG, et al. Am J Physiol Heart Circ Physiol. 2009 Mar;296(3):H815-22. PMID: 19136606.
Phytohemagglutinin is a lectin obtained from the red kidney bean that binds to the membranes of T-cells, stimulates metabolic activity and involves inflammatory pathways.
Apilimod is a potent IL-12/IL-23 inhibitor, and it is also a cell permeable small molecule which specifically inhibits PIKfyve with an IC50 of 14 nM in an in vitro kinase assay.
10-Hydroxy-trans-2-decenoic acid is the principal lipid component in royal jelly which is the food for queen and larvae honeybees.
Brij-35 (Polidocanol) is a high HLB, ethoxylated, nonionic ether of lauryl alcohol with broad pH stability.
Hyaluronic acid (HA) is an anionic, nonsulfated glycosaminoglycan distributed widely throughout connective, epithelial, and neural tissues.
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