Adjudin (also known as AF-2364) is a potent Cl- channel blocker, with a superior mitochondria-inhibitory effect. Adjudin inhibits cell proliferation in a dose dependent manner in SGC-7901 (human gastric adenocarcinoma cell), MDA-MB-231 (human breast adenocarcinoma cell), Smmc-7721 (human hepatoma cell) and MIA Paca-2 (human pancreatic adenocarcinoma cell) cells. The IC50 of Adjudin is determined to be 58.0 µM, 13.8 µM, 72.3 µM and 52.7 µM against SGC-7901, MDA-MB-231, Smmc-7721 and MIA Paca-2 cells, respectively, after treatment for 24 h. Similar results are obtained in other human and mice cancer cell lines. The IC50 of Adjudin in A549 cells and PC3 cells is 63.1 µM and 93.0 µM, respectively. Adjudin-treated mice show significant tumor growth inhibition compared with the control group (P<0.0001 in the human lung carcinoma cells A549 and P=0.006 in the prostate carcinoma cells PC3).
|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 sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans.
Li K, et al. Hum Reprod. 2013 Jan;28(1):47-59. PMID: 23117128.
|PLGA lactide:glycolide (75:25)
Poly(D,L-lactide-co-glycolide) is a synthetic amino acid that has been used to deliver macromolecular therapeutics.
|Icatibant (HOE 140)
Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor, with IC50 value of 1.07 nM and Ki value of 0.798 nM, respectively.
Guanidinoacetic acid (Glycocyamine) is a metabolic intermediate product of glycine in the human body, it is the direct precursor of creatine biosynthesis.
PF-04958242 is an α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid glutamate-positive allosteric modulator.
Poly-D-lysine is a positively charged amino acid polymer with approximately one HBr per lysine residue. The hydrobromide allows the poly-D-lysine to be in a crystalline form soluble in water.
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